Imipramine

It is an anti-arrhythmic drug and belongs to class IA of drugs.

Action:
It inhibits the reuptake of serotonin and norepinephrine.

Uses:
It is an anti-arrhythmic drugs and is also used in depression and enuresis in children aged 6 years.

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Worldwide Cancer Status

Cancer is found to be the leading cause of death in the world with the 13% of all death cases around the world in 2008. About 12.7 million cases of cancer and 7.6 million deaths were calculated in 2008. Upto middle-income countries there are about half (51%) of all cancer cases worldwide in 1975; while this proportion increased to 55% in 2007 and is thought to reach 61% by the year 2050.
There are more than 100 types of cancer and it can affect any part of the body.

Two factors are increasing the number of worldwide cancer patients:
1. Aging
2. Cancer causing attitude such as use of tobacco (It is estimated that about 1.3 billion people worldwide smoke tobacco), harmful or damaging use of alcohol, physical inactivity or poor diet
3. Older age
4. Race
5. Family history

Apart from these factors some other factors can also cause cancer such as
1. Over weight and obesity (WHO estimates that in 2005, overweight adults were about 1.6 billion from the total population and 300 million obese. It is estimated that the number of overweight people may go upto 2.3 billion by the year 2015.
2. Exposure to environmental carcinogens such as radon, arsenic, asbestos and polycyclic aromatic hydrocarbons.
3. Chronic Infections

A large number of cancer cases and deaths are in developing countries.More than 70 % of all cancer deaths occured in developing countries.
Breast Cancer is leading type of cancer in females and lung cancer is the leading type of cancer in males, since 1985, and they are also the leading cause of death from cancer for both developing as well as developed world. In females, lung cancer is the fourth most commonly diagnosed cancer and second most important cause of death from cancer. According to 2003-2007 research, top 5 cancer sites are prostate (a gland males that surround the tube for discharging urine located below the bladder), Breast, Lung as well as Bronchus and Colon (part of large intestine) as well as rectum (lower part of the large intestine).

Incidence rates of cancer is twice as high in developed countries as compared to developing countries.

It has been estimated that more than 30% of cancer deaths can be prevented by preventing the use of tobacco, taking a healthy diet, showing physical activity, and by prevention of infections that may cause cancer such as chronic (old) infections of hepatitis B virus (HBV) and/or human papillomavirus (HPV).

References:
Jemal, A.; Bray, F.; Center, M. M.; Ferlay, J.; Ward, E.; Forman, D. 2011. Global cancer statistics. A Cancer Journal for Clinicians, 61, Pages 69-90.

SEER Cancer Statistics Review 1975-2007. 2007. http://seer.cancer.gov/csr/1975_2007/browse_csr.php?section=1&page=sect_01_table.23.html#b . Accessed Mar 30, 2011.

Thun, M. J.; DeLancey, J. O. et al. 2010. The global burden of cancer: priorities for prevention. Carcinogenesis, Volume 31, Issue 1, Pages 100-110.
World Health Organization (WHO), Cancer; Fact Sheet. Feb 2011,  http://www.who.int/mediacentre/factsheets/fs297/en/ . Accessed Mar 30, 2011.

Nitroglycerin

It is also referred to as “Glyceryl trinitrate”.


Mechanism of action:
Intracellularly, Nitroglycerin gives nitrite ions, which then changes into endothelium derived relaxing factor (EDRF) i.e. nitric oxide. This NO then reacts with sulfhydryl (-SH) containing receptors associated with guanylate cyclase resulting in the activation of soluble Guanylate cyclase which promotes cells’ cyclic GMP level, which activates protein kinase G leading to the dephosphorylation of the myosin light chain. This causes ion binding process of Ca2+and at last relaxation of the vascular smooth muscle.

Actions:

It causes a reduced cardiac work resulting in the decreased oxygen demand of the heart muscles.

1. It causes venodilation so that blood is pooled in the veins resulting in the decreased preload and work of the heart.
2. It causes an increased flow of blood to the myocardium by dilating the coronary vessels.

Pharmacokinetics:
Its onset of action is one minute. It undergoes through the first pass metabolism and that is why it is taken sublingually or via transdermal patches.

Therapeutic uses:
Sublingual nitroglycerin is used for immediate relief from angina induced by physical activity or stress.

Nitrites and nitrates

These are nitric and nitrous acid esters of glycerol.

Mechanism of action:
1. Nitrates cause relaxation of the coronary vessels resulting in the decreased constriction of coronary vessels. The decreased constriction of the coronary arteries leads to increased transfusion of blood to the muscles of the heart (improved letting of blood).

2. On the other hand, it promotes dilation of the capacitance veins resulting in the decreased venous return to the heart due to pooled effect of blood in the veins. This decreased venous return to the heart decreases oxygen demand of the muscles of the heart.



Actions:

CVS:
Relaxation occurs in all segments of vascular system:
1. Less dilation of the arterioles and precapillary sphincters due to reflex responses.
2. They reduces cardiac output.

3. It effects directly on coronary artery tone resisting coronary artery spasm in variant angina.


4. Organonitrates causes relaxation of the arteries resulting in the reduced systemic arterial pressure causing reduced afterload of the heart leading to the reduced cardiac oxygen requirement.

5. Organonitrates causes relaxation of the veins resulting in the reduced preload causing reduced myocardial wall tension leading to reduced myocardial oxygen requirement.

6. Reduced left ventricular end diastolic volume reduces tissue pressure around subendocardial vessels  promoted coronary blood flow to this area

Other smooth muscle organs:
Organonitrates have short duration of action on the relaxation of the smooth muscles i.e. esophageal and biliary smooth muscle.

Blood:
Nitrite ion may cause pseudocyanosis and tissue hypoxia.

Therapeutic uses:
1. Stable and unstable angina pectoris
2. Variant angina pectoris
3. Orthopnea and Paroxysmal nocturnal dyspnea
4. Cyanide poisoning

Adverse effects:
Facial flushing (due to cutaneous vasodilation), Severe type of headache (due to vasodilation of cerebral vessels leading to elevated intracranial pressure and headache), Orthostatic hypotension, dizziness, weakness

Nadolol

This has a long duration of action.


Therapeutic uses:
1. Hypertension
2. Angina pectoris
3. Cardiac tachyarrhythmias

Implants

This represents the form of radiation therapy or radiotherapy involving placement of radioactive entities inside the body of the patient close to the tumor.

An artificial body part placed in tissues (often to replace missing body parts) with the help of surgery.

Fusion protein

Fusion proteins are produced by the combination of two genes or proteins or peptides. They can exist naturally or can be prepared in the laboratory.

PEGylated dosage forms

PEGylated dosage form refers to the attachment of the polythylene glycol polymer chains to a drug concealing the agent from the immune sytem of the body reducing immunogenicity resulting in prolonged circulatory time.

Examples:
PEGylated interferon alpha is in use for the treatment of hepatitis B and C.
PEGylated liposome having doxorubicin is used in the treatment of cancer.

Ophthalmic Inserts

Ophthalmic inserts are solid or semisolid sterile preparations for placement in the conjunctival sac of the eye. These are sustained release drug delivery systems for the eye.

Osmotic Systems

Osmotic systems make use of osmotic pressure for controlled delivery of active ingredients.
This method can be used both for systemic and targeted drug delivery.

Mechanism:
Osmotic pressure as a result of imbibitions of the fluid by the osmotic agents directly affects the rate of drug delivery from osmotic systems such as osmotic pumps.

Components of Osmotic Pump:
1. Drug
2. Osmotic agent or osmogent such as magnesium sulfate, sodium chloride or sodium bicarbonate
3. Semipermeable membrane
4. Plasticizers such as polyethylene glycols, triethyl citrate or ethylene glycol monoacetate

Factors affecting Osmotic drug delivery:
1. Size of the opening of delivery point
2. Solubility of the components
3. Intrinsic character of the rate controlling membrane
4. Osmotic pressure of the components

These factors are important to develop an optimized and desired osmotic system.

Mucoadhesive system

Mucoadhesion refers to adhesion with with moist lining in the body passages of mammals containing cells which secrete mucus and opens to the external environment.

Mucoadhesive system refers to the adhesion of natural or synthetic polymer and soft tissues of mucous membrane for an extended period. Cross linked polymer device, containing drug, will adhere to biological membrane and will transfer the drug to the body at the given site, decreasing frequency of administration.

Theories of mucoadhesion:
Following theories have been proposed in the mucoadhesion of the drug:
1. The wetting theory
2. The diffusion theory
3. The electronic theory
4. The adsorption theory
5. The cohesive theory
6. The Fracture theory
7. The mechanical theory

Controlled release microchips

It represents the slow and controlled release of medicaments from microfabricated device. These are the types of small programmable devices.

In this microchip, micrometer scale pumps, valves and flow channels are incorporated or microfabricated into the active devices. Microchip of solid state silicon can be used in this technique. These microchips have following properties:

1. They can store a large amount and number of chemicals or medicaments
2. They have the ability of controlling the time of release of chemicals or medicaments
3. They have the ability of controlling the rate of release of chemicals or medicaments

These microchips have a tiny power supply. The control of microchips are done by remote control, microprocessors and/or biosensors.

The chemical release takes place through electrochemical dissolution of membranes of thin anode covering microreservoirs which are filled with chemicals in the form liquid, solid or gel.

Uses:
This microchip technology has found uses in many areas such as chemical detection, drug delivery, medical diagnostics and combinatorial chemistry.

References:
January 20, 1999. A commentary on the controlled release microchip. http://web.mit.edu/newsoffice/1999/microchipcom.html. Accessed March 28, 2011.
Santini, J. T. Jr.; Cima, M. J.et al. 1999. A controlled-release microchip. Nature, 397, Pages 335-338.

Santini, J. T. Jr.; Richards, A. C. et al. 2000. Microchips as Controlled Drug-Delivery Devices. Wiley-VCH, 39, Pages 2396-2407.

Phonophoresis

It represents the use of ultrasound for the delivery of drugs through the skin. Through this process topical application of anti-inflammatory drugs and analgesics can be increased.

Iontophoresis

A therapeutic strategy or technique in which a small amount of electric current is used locally for introduction of of medicine or some other chemicals (heavy metal ions) into the tissues of the body through the skin.

In this process, bipolar electrodes are used to create electric potential and ionized medication is introduced into the body. Moreover, sweat glands temporarily turn off during this procedure.

Moxalactam

It is also known as Latamoxef. It is a third generation cephalosporin and is used parenterally.

Uses:It is a active against Enterobacteriaceae. It is used in the treatment of complicated urinary tract infections.

Ceftriaxone

It is a third generation cephalosporin and is administered parenterally.

Action:
It inhibits mucopeptide synthesis in the bacterial cell wall.

Uses:
It is used for the treatment of infections of skin, respiratory tract and urinary tract.

Ceftizoxime

It is a third generation cephalosporin and is administered parenterally or in the form of suppository.

Action:
It binds to specific penicillin binding protein and inhibits cell wall synthesis.

Uses:
It is effective against susceptible strains of micro-organisms.

Ceftazidime

It is a third generation cephalosporin and is administered parenterally.

Action:
It binds to specific penicillin binding protein and inhibits cell wall synthesis.

Uses:It is used to treat infections caused by Pseudomonas and other gram negative infections.

Cefotaxime

It is a third generation cephalosporin. It is administered parenterally.

Action:
It binds to specific penicillin binding proteins in the cell wall of bacteria and inhibits bacterial cell wall synthesis.

Uses:It is used to treat infections of meningitis, gonorhoea and infections of the kidney.

Cefoperazone

It is a third generation cephalosporin. It is administered parenterally.

Action:
It binds to specific penicillin binding proteins and inhibits cell wall synthesis.

Uses:It is especially used for the treatment of infections caused by the species of Pseudomonas.

Cefixime

It is a third generation cephalosporin and is administered parenterally.

Action:
It inhibits cell wall synthesis by binding to penicillin binding proteins.

Uses:
It is used to treat uncomplicated urinary tract infections and otitis media.

Cefmenoxime

It is a third generation cephalosporin.

Action:
It binds to penicillin binding protein and inhibits bacterial protein synthesis.

Uses:It is effectively used to treat obstetric and gynecologic infections.

Cefetamet

It is a third generation cephalosporin.

Uses:It is active against Enterobacteriacae, streptococci and haemophilis.

Cefsulodin

It is a 3rd generation cephalosporin.

Uses:It is used to treat infections caused by P. aeruginosa.

Cefpiramide

It is a 3rd generation cephalosporin.

Action:
It binds to penicillin binding protein.

Uses:It is effective against infections caused by P. aeruginosa.

Cefpimizole

It is a third generation cephalosporin. It is a semisynthetic antibiotic and is used parenterally.

Latamoxef

It is a third generation cephalosporin and is a beta lactam antibiotic.

Action:
It inhibits bacterial cell wall synthesis.

Uses:
It is used to treat infections of meninges, urinary tract and gastrointestical tract.

Flomoxef

It is a third generation cephalosporin. It is active against pathogenic Nocardia.

Ceftiolene

It is a third generation cephalosporin. It is similar to ceftriaxone or cefotaxime.

Ceftibuten

It is a 3rd generation cephalosporin. It is administered orally.

Action:
It inhibits bacterial cell wall synthesis.

Uses:
It is used to treat chronic bronchitis, pharyngitis and tonsilitis.

Cefteram

It is a 3rd generation cephalosporin. It can be administered orally.

Cefpodoxime

It is a third generation cephalosporin.

Action:
It binds to penicillin binding protein and results in inihibition of cell wall synthesis.

Uses:
It is used for upper and lower respiratory tract infections and urinary tract infections.

Cefodizime

It is a third generation cephalosporin. It is used parenterally.

Uses:It is used for respiratory tract infections and urinary tract infections.

Cefditoren

It is a 3rd generation cephalosporin.

Action:
It acts on penicillin binding protein and results in inhibition of cell wall synthesis.

Uses:
It is used for community acquired pneumonia, chronic bronchitis and pharyngitis.

Cefdinir

It is a 3rd generation cephalosporin.

Action:It acts on penicillin binding proteins resulting in the inhibition of bacterial cell wall synthesis.

Uses:
It is effective in the treatment of common infections of bacteria such as that of ear, throat and sinus.

Cefdaloxime

It is a third generation cephalosporin.

Cefcapene

It is 3rd generation cephalosporin.

Action:
It is a beta-lactamase inhibitor.

Uses:It is used to treat chronix respiratory tract infections.

Loracarbef

It is a second generation cephalosporin and is administered parenterally.

Action:
It is a beta lactam antibiotic and works by binding to penicillin binding proteins.

Uses:It is used for bacterial infections, pneumonia, pharyngitis and urinary tract infections.

Cefuroxime

It is a second generation cephalosporin and is administered parenterally.

Action:
It is a beta lactam antibiotic and works after binding to penicillin binding protein.

Uses:
It is used for both of the gram positive and gram negative organisms and is helpful in the treatment of gonorhea and haemophilus.

Cefprozil

It is a second generation cephalosporin and is administered parenterally.

Action:
It is a beta lactam antibiotic and it works after binding with penicillin binding proteins.

Uses:
It is used to treat bronchitis, skin infections and other bacterial infections.

Cefotetan

It is a second generation cephalosporin and is administered parenterally.

Action:
It caused inhibition of cell wall synthesis of the bacteria by binding and inhibiting the penicllin binding proein.

Uses:
It is active against a wide range of aerobic and anaerobic, gram positive and gram negative micro-organisms.

Cefoxitin

It is a second generation cephalosporin and is administered parenterally.

Action:
It inhibits bacterial cell wall synthesis.

Uses:
It is used against infections caused by susceptible bacteria.

Ceforanide

It is a second generation cephalosporin and is administered parenterally.

Action:
It causes inhibition of cell wall synthesis.

Uses:
It is used for the infections caused by susceptible bacteria.

Cefonicid

It is a second generation cephalosporin and is administered parenterally.

Action:It inhibits cell wall synthesis by binding to penicillin binding proteins.

Uses:It is used for lower respiratory infections, urinary tract infections and soft tissue and bone infections.

Cefmetazole

It is a second generation cephalosporin and is administered parenterally.

Action:It causes inhibition of cell wall synthesis.

Uses:It is used in the treatment of infections caused by susceptible organisms.

Cefamandole

It is a second generation cephalosporin and is administered parenterally.

Action:
Like other cephalosporins, it also works after binding with penicillin binding proteins.

Cefaclor

It is a second generation cephalosporin. It is administered orally.

Action:It inhibits cell wall synthesis by binding to penicillin binding proteins.

Uses:It is used to treat pneumonia and infections of skin, lungs and urinary tract.

Cefuzonam

It is a second generation cephalosporin.

Action:
It binds to penicillin binding protein and inhibits cell wall synthesis.

Cefbuperazone

It is a second generation cephalosporin. It is similar in activity to moxalactam.

Cefotiam

It is a second generation cephalosporin.

Action:
It inhibits cell wall synthesis as it binds to penicillin binding proteins

Uses:
It is used to treat infections caused by susceptible bacteria.

Cefminox

It is a second generation cephalosporin. It is a very effective beta lactam antibiotic.

Uses:It is used to treat respiratory and urinary tract infections.

Cefazolin

It is a first generation semisynthetic cephalosporin administered parenterally.

Action:
It is used to inhibit cell wall synthesis.

Uses:It is used to treat infections of the skin.

Cefapirin

It is a first generation cephalosporin administered parenterally.
Action:
It acts on penicillin binding proteins and resulting in the inhibition of cell wall synthesis.

Uses:
It is used to treat infections caused by susceptible bacteria.

Cefalothin

It is a first generation cephalosporin administered parenterally.

Action:
It causes inhibition of cell wall after binding to penicillin binding proteins.

Uses:
It is used to treat urinary tract infections, respiratory infections and infections during surgery.

Cefaloridine

It is a first generation cephalosporin administered parenterally.

Cefradine

It is a first generation semisynthetic cephalosporin. It is similar in activity to cefalexin.

Cefalexin

It is a first generation semisynthetic cephalosporin. It is taken orally.

Action:It is a beta lactam antibiotic and binds to penicllin binding protein in the cell wall resulting in the inhibition of cell wall.

Uses:
It is used for the treatment of respiratory tract infections and genitourinary tract infections.

Cefadroxil

It is a first generation cephalosporin taken orally.

Action:It binds to penicillin binding protein in bacterial cell wall and inhibits cell wall synthesis.

Uses:It is used for the infections caused by H. influenzae, S. pneumoniae and E. coli such as urinary tract infections, pharyngitis and tonsilitis.

Ceftezole

It is a first generation cephalosporin.

It inhibits cell wall synthesis.

Cefroxadine

It is a first generation cephalosporin. It is very similar to cefalexin in structure and mode of activity.

Cefazaflur

It is a first generation cephalosporin. It is a semisynthetic cephalosporin.

Cefazedone

It is a 1st generation cephalosporin. It is related to penicillin.

Action:
It causes inhibition of mucopeptide synthesis in the cell wall.

Classifications in Pharmacy (CIP) Software

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This software strictly requires ".NET Framework 3.5". Download from the following links:
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Cefatrizine

It is a 1st generation cephalosporin. It is taken orally or intramuscularly.

Uses:It has broad spectrum antibiotic activity.

Cefaloglycin

It is a 1st generation cephalosporin.

Action:
It binds to penicillin binding protein and results in the inhibition of cell wall synthesis in bacteria.

Uses:
It is used for serious infections caused by susceptible bacteria.

Cefacetrile

It is a 1st generation cephalosporin. It is derived from 7-aminocephalosporanic acid.

Action:
It binds to specific penicillin binding proteins and causes inhibition of cell wall synthesis.

Uses:It is effective against Gram positive and Gram negative bacteria.

Anesthetic machine

A machine or device helping in the administration of anesthesia.

Oxygen Mask

A device used for the delivery of oxygen from a storage tank to the lungs.

Dry Powder Inhaler

It is a device for inhalation of the dry powder used to treat respiratory disease.

Pessary

A small medical device made of silicone or plastic and is inserted into the rectum or vagina. It may be used as a contraceptive or for the support of uterus.

Douche

It refers to a device with detachable nozzles used for introducing a stream of water into the body cavity for medical or hygienic purposes.

Enema

It refers to the administration of a liquid through anus in order to evacuate it. It is usually used for the treatment of constipation.

Lotion

A slightly viscous medicated topical preparation used for application on the skin. It may have soothing or antispetic use.

Liniment

A topical medicated liquid used to remove muscular pain or stiffness by rubbing into the skin.

Intraosseous

It refers to the injection directly into the bone marrow.

Intracardiac

It refers to the injection directly into the muscles or ventricles of the heart.

Intraperitoneal

It refers to the injection of a substance into the lining of the abdominal cavity.

Intravenous

It refers to within or through veins.

Intramuscular

It refers to wihtin a muscle.

Epidural

It refers to the space around the spinal cord where spinal fluid circulates.

Intracerebral

It refers to within the brain.

Intrathecal

It refers to inside of the spinal canal.

Transscleral

It refers to across the white (sclera) of the eye.

Intracavernous

It refers to injection into the base of the penis.

Intravitreal

It refers to the administration of the drug throught the eye.

Transdermal

It refers to the administration through the unbroken skin in the form of a patch.

Intradermal

It refers to the areas between or within the layers of the skin.

Subcutaneous

It refers to below the epidermis.

Inhaler

It is a device for inhalation of medicated vapors to relieve nasal congestion, asthma and chronic obstructive pulmonary disease (COPD).

Aerosol

It represents the suspension of tiny solid or liquid particles, especially medicated particles, in a gaseous environment. The size of the particles may range from 1 nanometer or 100 micrometers.

Vaporizer

A device that converts the substance to vapor form used specially for medical purposes.

It is used for delivery of the active ingredients in the form of inhalation.

Pressurized metered dose inhaler

It is abbreviated as pMDI. It is a device for administration of a particular amount of medicine to the lungs.

It is most commonly used in the management of asthma.

Nebulizer

It is also referred to as atomizer. A device such as mask or mouthpiece that turns the liquid into condensed water vapor or fine mist for inhalation into the lungs.

It is often given in the delivery of asthma medications.

Toothpaste

A tooth cleaning compound used in the form of paste.

Mouthwash

A medicated solution used for rinsing and gargling the mouth resulting in increased oral hygiene.

Lozenge

It is a type of candy or small pellet which is medicated or aromatic. It is intended for slow dissolution in the mouth and often a demulcent is used in lozenges i.e. a substance helpful in soothing the mucus membrane which is inflamed.

Cefpirome

It is a 4th generation cephalosporin.

Action:
It binds to penicillin binding protein and inhibits peptidoglycan synthesis in bacterial cell wall.

Uses:
It is active against gram positive and gram negative bacteria and is used for the treatment of lower respiratory tract infections and upper and lower urinary tract infections.

Cefozopran

It is a 4th generation cephalosporin. It is used parenterally.

Uses:
It is used against respiratory tract infections and urinary tract infections.

Cefepime

It is a 4th generation cephalosporin.

Action:
It has same action as that of other beta lactam antibiotics such as penicillin.

Uses:
It has an extended spectrum of activity against gram-positive and gram-negative bacteria and is used for the treatment of pneumonia and urinary tract infections.

Ceftobiprole

It is a fifth generation cephalosporin.

Action:
It inhibits penicillin binding proteins.

Uses:
It is used against infections caused by staphylococcus, streptococcus and enterococci.

Telithromycin

It is a ketolide antibiotic. It is derived from erythromycin.

Action:
It binds to 23S rRNA of the 50S ribosomal subunit of the bacteria having 25 times more affinity for macrolide resistant strains.

Uses:
It is used for the treatment of acute sinusitis, acute bronchitis and acute bacterial tonsilitis.

Cethromycin

It is a ketolide antibiotic.

Uses:It is an orphan drug for the treatment of post exposure inhalational anthrax. Research is on the way for its use in community acquired pneumonia (CAP).

Ansamycin

It is a ketolide antibiotic.

Action:
It inhibits DNA dependent RNA polymerase activity.

Uses:
It is used against many gram positive bacteria and some gram negative bacteria.

Sorangicin-A

It is a broad spectrum macrolide antibiotic. It is isolated from Sorangium cellulosum.

Quinopristin/dalfopristin

It is a macrolide antibiotic.

Action:
Dalfopristin binds to 23S portion of 50S ribosomal subunit and Quinopristin binds to a nearby site of 50S ribosomal subunit and in this way they causes the inhibition of protein synthesis.

Uses:It is used for the treatment of Staphylococcal infections and infections caused by Enterococcus faecium.

Pristinamycin

It is a macrolide antibiotic.

Uses:It is used in the treatment of staphylococcal infections and to some extent for streptococcal infections.

Lincomycin

It is a macrolide antibiotic.

Mechanism of Action:
It binds to 50S ribosomal subunit of bacteria and results in decreased protein synthesis.

Uses:It is used in the treatment of infections caused by staphylococcus and streptococcus.

Clindamycin

It is a macrolide antibiotic.

Mechanism of Action:
It binds to 50S ribosomal subunit of bacteria resulting in decreased protein synthesis.

Uses:It is used for osteomyelitis, dental infections and diabetic foot ulcers.

Maridomycin

It is a macrolide antibiotic.

Uses:It is an antibiotic and is also used for the Uterine myoma and endometriosis.

Kejanimicin

It is a macrolide antibiotic and is structurally related to tetrocarcin.
Kejanolide is the aglycon portion of the Kajanamicin.

Tetrocarcin

It is a macrolide antibiotic.

Action:
It inhibits Bcl2 function and thereby inhibiting the anti-apoptic activity.

Uses:It is an antibiotic with a strong antitumor activity.

Chlorothricin

It is a macrolide antibiotic.

Flurithromycin

It is macrolide antibiotic. It is a derivative of Erythromycin and is also similar in action to erythromycin.

Rokitamycin

It is a macrolide antibiotic.

Action:
It causes inhibition of the protein synthesis.

Uses:It is effectively used in the infections caused by Gram positive bacteria, E. faecalis and H. influenzae.

Miocamycin

It is a macrolide antibiotic.

Uses:It is effective in respiratory and genital infections.

Carbomycin-A

It is an similar to erythromycin.

Action:
It causes the inhibition of protein synthesis.

Troleandomycin

It is a macrolide antibiotic.It is similar to erythromycin.

Action:
It binds to 50S ribosomal subunit of bacteria resulting in inhibition of protein synthesis.

Uses:
It is used for the treatment of Pneumococcal pneumonia.

Spiramycin

It is a macrolide/ketolide antibiotic. It is an experimental drug.

Uses:It is used to treat toxoplasmosis.

Oleandomycin

It is a macrolide/ketolide antibiotic.

Uses:
It is used in the infections caused by Bacillus subtilis, Enterococcus faecalis and Staphylococcus aureous.

Midecamicin

It is a macrolide antibiotic.

Uses:
It inhibits staphylococci, streptococci and some species of Hemophilus.

Kitasamycin

It is a macrolide antibiotic. It is used against a wide spectrum of pathogens.

Leucoscandrolide B

It is a macrolide antibiotic.

Josamycin

It is a macrolide antibiotic. It is used against a wide spectrum of pathogens.

Mechanism of Action:
It binds reversibly to 50S ribosomal subunit of bacteria resulting in the inhibition of translocation of peptidyl tRNA.

Leucascandrolide A

It is macrolide antibiotic.It is a biologically active marine natural product.

Roxithromycin

It is a macrolide antibiotic.It is similar in action to erythromycin or azithromycin.

Dirithromycin

It is a macrolide antibiotic.

Mechanism of Action:
It binds to the 50S ribosomal subunit of bacteria resulting in the inhibition of the translocation of the peptides.

Uses:
It is used to treat bacterial infections such as tonsillitis, bronchitis and pneumonia.

Erythromycin

It is a macrolide antibiotic.

Mechanism of Action:
It inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit.

Uses:
It is used for the treatment of respiratory tract infections and pertussis.

Clarithromycin

It is a Macrolide antibiotic derived from erythromycin.

Mechanism of Action:
It inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit.

Uses:It is used for the treatment of acute otitis media and infections caused by H. influenzae and S. pneumoniae.

Azithromycin

It is a macrolide antibiotic.

Action:
It binds to 50S ribosomal subunit of bacterial ribosome resulting in the inhibition of the peptidyl transferase activity.

Uses:
It is used for the infections caused by H. Influenzae, C. Pneumoniae and S. aureus.

Vertilmicin

It is an aminoglycoside antibiotic. It is structurally very similar to netilmicin.

Uses:It is a potent bactericidal agent against E. coli, S. aureus and Klebsiella pneumoniae.

Tobramycin

It is an aminoglycoside antibiotic.

Action:
It binds to 30S ribosomal subunit inhibiting bacterial protein synthesis.

Used:
It is used in the treatment of infections caused by gram negative bacteria especially pseudomonas species.

Sisomicin

It is an aminoglycoside antibiotic derived from "Micromonospora" bacteria. It is closely related to gentamicin.

Uses:It is used in the treatment of the infections caused by Serratia and indole positive Proteus species.

Ribostamycin

It is an aminoglycoside antibiotic.

Mechanism of Action:
It binds to 30S ribosomal subunit of bacteria resulting in the reduction of the synthesis of the bacterial proteins.

Paromomycin

It is an aminoglycoside antibiotic.

Action:
It inhibits bacterial protein synthesis by binding to 16S rRNA.

Uses:It is used for the treatment of both acute as well as chronic intestinal amebiasis.

Netilmicin

It is an aminoglycoside antibiotic.It is derived from sisomycin and is similar in action to gentamicin.

Isepamicin

It is an aminoglycoside antibiotic similar in action to amikacin.

Habekacin

It is an aminoglycoside antibiotic.

It is similar in action to kanamycin and gentamicin.

Framycetin

It is an aminoglycoside and is a component of neomycin.

Mechanism of Action:
It binds to 30S subunit proteins and 16S rRNA resulting in the production of nonfunctional peptides.

Uses:It is used for the treatment of bacterial blepharitis and corneal injuries. It is also used for the treatment of Conjunctivitis.

Dibekacin

It is an aminoglycoside antibiotic.It is derived from Kanamycin B.

Uses:
It is used in the infections of E. coli and P. Aeruginosa.

Amikacin

It is an aminoglycoside antibiotic derived from Kanamycin A.

Action:
It binds to 30S ribosome of susceptible organism resulting in the inhibition of bacterial protein synthesis.

Uses:
It is used for the treatment of severe infections caused by Gram Negative Organisms including E. coli and Pseudomonas species.

Verdamicin

It is an aminoglycoside derived from "Micromonospora" bacteria.

It is similar to gentamicin.

Gentamicin

It is an aminoglycoside antibiotic derived from "Micromonospora" bacteria.

Mechanism of Action:
It binds irreversibly to 30S-subunit proteins and 16S rRNA resulting in the production of nonfunctional peptide.

Uses:
It is used to treat infections caused by E. coli and proteus species.

Spectinomycin

It is an aminoglycoside antibiotic derived from "Streptomyces" bacteria.

Mechanism of Action:
It acts on 30S ribosomal subunit resulting in the inhibition of the protein synthesis in the bacterial cell wall.

Uses:
It is used for the treatment of gonorrhea.

Hygromycin B

It is an aminoglycoside antibiotic derived from "Streptomyces" bacteria.

Action:
It inhibits polypeptide synthesis.

Kanamycin

It is an aminoglycoside derived from "Streptomyces" bacteria.

Action:
It binds irreversibly to 30S ribosomal subunit proteins and 16S rRNA. This results in the non-functional peptides.

Uses:It is used for the treatment of infections caused by E.coli and proteus species.

Neomycin

It is an aminoglycoside derived from "Streptomyces" bacteria.

Action:
It binds to 30S ribosomal subunit and resulting in the production of non-functional peptide.

Uses:
It is used topically for the treatment of superficial eye infections and may be used orally for the treatment of hepatic encephalopathy.

Streptomycin

It is an aminoglycosides derived from "Streptomyces" bacteria.

Action:
It causes disruption in the initiation and elongation steps in protein synthesis by binding to the 30S ribosomal subunit of the the susceptible organism.

Mainly active against extracellular tubercle bacilli as it penetrates poorly into cells.

Uses:
It is used for the treatment of tuberculsosis.

Adverse effects:It is ototoxic and nephrotoxic. It may also cause vertigo and hearing loss.

Sulfasalazine

It is an antibacterial sulfonamide.

Uses:
It is used in the treatment of inflammatory bowel disease. It is also used in the treatment of rheumatoid arthritis.

Phthalylsulfathiazole

It is a antibacterial sulfonamide.

Action:
It inhibits the bacterial enzyme dihydropteroate synthetase.

Uses:
It is used to treat intestinal infections.

Sulfapyridine

It is a topical sulfonamide.

Action:
It competitively inhibits the bacterial enzyme dihydropteroate synthetase resulting in the inhibition of folic acid in bacteria.

Uses:
It is an anti-bacterial used to treat pyoderma gangrenosum and dermatitis herpetiformis.

Silver Sulfadiazine

It is a topical sulfonamide.

Action:It acts on the cell wall and cell membrane to produce a bactericidal effect.

Uses:
It is used as an adjunct in the treatment of second and third degree burns.

Mafenide

It is a topical sulfonamide.

Action:
It decreases the bacterial population  and increases the healing around the burns.

Uses:
It is used as an adjunctive treatment for serious burns.

Xipamide

It is a sulfonamide diuretic.

Action:
It decreases sodium reabsorption in the distal convoluted tubule.

Uses:
It is a thiazide like diuretic and is also used in the treatment of hypertension and edema.

Metolazone

It is a sulfonamide diuretic. It is a quinazoline derivative.
Action:
It inhibits sodium reabsorption at cortical diluting site.

Uses:
It is thiazide like diuretic and causes an increase in potassium loss. It is also used in lowering blood pressure.

Mefruside

It is a sulfonamide diuretic.

Uses:
It is a diuretic and is also used for the treatment of hypertension and edema.

Indapamide

It is a sulfonamide diuretic. It is a lipid soluble nonthiazide diuretic related to indolines.
Action:
It inhibits the slow component of delayed rectifier potassium current.

Pharmacokinetics:

It has a long duration of action. It is metabolized by the gastrointestinal tract and excreted by the kidneys.


Uses:
It is a thiazide like diuretic used orally and is also used in the treatment of hypertension and edema.

Hydrochlorothiazide

It is a sulfonamide diuretic. It is similar to chlorothiazide.
Action:
It inhibits sodium-chloride symporter in the distal convoluted tubule resulting in the inhibition of the water reabsorption.

Uses:
It is a thiazide diuretic and is used in the treatment of edema and high blood pressure.

Furosemide

It is a sulfonamide diuretic. Its chemical name is 4-Chloro-N-furfuryl-5-sulfamoylanthranilic acid.
Action:
It blocks sodium-potassium-chloride cotransporter in thick ascending limb of the loop of Henle resulting in the inhibition of the water reabsorption. It increases renal blood flow and causes redistribution of blood flow within renal cortex.

Administration and dosage:

Furosemide can be administered orally, IM or intravenously. Its usual dosage is 20-50 mg per day.
Pharmacokinetics:
It is excreted renally. Its onset of action is 30 minutes to 60 minutes and duration of action is 2 hours (when administered IV) and 6-8.5 hours (when administered orally).

Therapeutic uses:
1. Edematous states from congestive heart failure or some renal disease
2. Hypertension
3. To increase serum calcium level
4. It is a diuretic.

Adverse effects:
Light-headedness, dizziness, thirst, weakness

Interaction:
Furosemide and bumetanide weakly inhibit carbonic anhydrase.

Dorzolamide

It is a sulfonamide diuretic.

Action:
It is a carbonic anhydrase inhibitor.
Uses:
It is used as a diuretic. It is also used in glaucoma and hypertension relating to eyes.

Clopamide

It is a piperidine sulfonamide diuretic.

Action:
It works in the similar way as thiazide diuretics.
Uses:
It is used as diuretic.

Chlorthalidone

It is a thiazide like diuretic sulfonamide.

Action:
It causes inhibition of the transport of the sodium ions across the renal tubular epithelium in the ascending limb of the loop of Henle.

Pharmacokinetics:
It has long duration of action, so given once per day..

Uses:
It is used as a diuretic in the treatment of hypertension.

Dichlorophenamide

It is a diuretic sulfonamide.

Action:
It is a carbonic anhydrase inhibitor.
Uses:
It is used as diuretic.Its most important use is in the treatment of glaucoma.

Methazolamide

It is a diuretic sulfonamide.

Action:
It is a strong and effective inhibitor of Carbonic anhydrase.
Uses:
It is used as diuretic and in the treatment of glaucoma.

Ethoxzolamide

It is a diuretic sulfonamide.

Action:
It binds to and causes inhibition of the enzyme carbonic anhydrase I.
Uses:
It is used as diuretic. It is also used in glaucoma.

Bumetanide

It belongs to the class of diuretic sulfonamide. It is a metanilamide derivative.


Action:
It interferes with renal cAMP and/or results in the inhibition of the sodium/potassium ATPase pump. It causes dilation of blood vessels in the kidneys and thus increases renal blood flow.

Pharmacokinetics:
Its half life is 1-1.5 hour. Its onset of action is 30 minutes to 90 minutes and duration of action is 4-6 hours.

Uses:
It is used as diuretic and can also be used in the treatment of edema associated with congestive heart failure. It is also used for Hepatic Cirrhosis.

Adverse effects:
Nausea, vomiting, rashes and abdominal pain

Interaction:
Furosemide and bumetanide weakly inhibit carbonic anhydrase.

Benzolamide

It is a diuretic sulfonamide and is an orphan drug.

It is similar to acetazolamide.

Action:
It is a carbonic anhydrase inhibitor.

Uses:
It is used as diuretic and can be used in the cases of respiratory failure.

Acetazolamide

It is a diuretic sulfonamide.

Action:
It is a carbonic anhydrase inhibitor.

Uses:
It is used in the treatment of epileptic seizures, glaucoma, edema due to congestive heart failure and diuretic.

Sulfaphenazole

(It is in experimental stages.)

It is a long acting sulfonamide antibacterial.

Action:
It specifically inhibits CYP2C9 i.e an important cytochrome P450 enzyme important in the oxidation of endogenous compounds.

Sulfametopyrazine

(It is now withdrawn)
It is a long acting sulfonamide.

Action:
It competitively inhibits the bacterial enzyme dihydropteroate synthetase.

Uses:
It is used for Urinary tract infections, Respiratory tract infections and malaria.

Sulfamethoxy-pyridazine

It is a long acting sulfonamide.

Uses:
It is used to treat Urinary Tract Infections, Pneumonia and bronchitis.

Sulfadoxine

Sulfadoxine is an intermediate to long acting sulfonamide.

Uses:
It is generally used in combination with other drugs

Sulfacetamide

It is an intermediate acting sulfonamide and is available in the salt form alongwith sodium.

Mechanism of Action:
It competitively inhibits the bacterial enzyme para-aminobenzoic acid resulting in the inhibition of the synthesis of the folic acid.

Uses:
It is used in the treatment of skin infections and orally it is useful in the treatment of Urinary tract infections.

Sulfisomidine

It is also known as sulfasomidine and it is a short acting sulfonamide.

It is similar to sulfadimidine.

Sulfisoxazole

It is a short acting sulfonamide.

Mechanism of Action:
It inhibits the folic acid production of bacteria by competitive inhibition of the enzyme dihydropteroate synthetase.

Uses:
It is used for the treatment of Urinary Tract Infections, Acute otitis media, meningococcal meningitis, malaria and other bacterial infections.

Sulfamethoxazole

It is a short acting bacteriostatic sulfonamide.

Action:
It hinders folic acid synthesis in susceptible bacteria.

Uses:
It is used to treat prostatitis, bronchitis and Urinary tract infections.

Brand Names:
•Apo-Sulfamethoxazole

•Azo Gantanol
•Azo-Gantanol
•Bactrimel
•Gamazole
•Gantanol
•Gantanol-DS
•Metoxal
•Radonil
•Septran
•SIM
•Simsinomin
•Sinomin
•Sulfamethalazole
•Sulfamethoxazol
•Sulfamethoxizole
•Sulfamethylisoxazole
•Sulfisomezole
•Sulpha-Methoxizole
•Sulphamethalazole
•Sulphamethoxazol
•Sulphamethoxazole
•Sulphamethoxazole BP 98
•Sulphamethylisoxazole
•Sulphisomezole
•Trib
•Urobak

Sulfamethizole

Sulfamethizole is a short acting sulfonamide antibiotic.

Mechanism of Action:
It inhibits the bacterial enzyme dihydropteroate synthetase.
Uses:
It is used for the treatment of Urinary Tract Infections.

Sulfadimidine

It is also known as Sulfamethazine and it is a sulfonamide antibiotic. It is a short acting sulfonamide.

Uses:
It is used to treat lower urinary tract infections and meningococcal meningitis.

Sulfadiazine

It is a sulfa drug i.e. sulfonamide antibiotic.

Mechanism of Action:
It stops the production of folic acid in the cell wall of bacteria.

Action:
It is short acting sulfonamide.

Uses:
It is used in the treatment of pneumonia, meningitis, urinary tract and other infections.

Tacrine

Tacrine is available in the form of Tacrine hydrochloride.

Action:It is a parasympathomimetic and acts centrally as an anticholinesterase.

Uses:
It is used in the treatment of mild to moderate Alzheimer's disease as it causes memory improvement.

Rivastigmine

It is available in the salt form of Rivastigmine tartarate.

Action:
It is a parasympathomimetic (cholinergic) agent.

Uses:
It is used in the treatment of mild to moderate dementia caused by Alzheimer's disease or Parkinson's disease.

Physostigmine

Physostigmine is avalaible in the salt form of Physostigmine hydrochloride and Physostigmine Salicylate. It is a parasympathomimetic and is a reversible cholinesterase inhibitor.

Uses:
It is used in the treatment of Alzheimer's disease. It is also used for the treatment of glaucoma.

Memantine

Mematine is available in the salt form as a compound of Memantine hydrochloride.

Mechanism of Action:
Memantine is an N-methyl-D-Aspartate (NMDA) receptor antagonist.

Uses:
It is used in the management of Alzheimer's disease.

Galantamine

It is available in the salt form of Galantamine Hydrobromide.

Action:
It is an acetylcholinesterase inhibitor working additionally on acetylcholine receptor in this way it not only inhibits breakdown of acetylcholine but also results in its distribution.

Uses:
It is used in the treatment of mild to moderate Alzheimer's disease and various memory impairments.

Donepezil

It is available in the salt form of Donepezil Hydrochloride.

Mechanism of Action:
It is a centrally acting reversible acetylcholinesterase inhibitor resulting in an increased action of acetylcholine by inhibiting its break down by the cholinesterase enzyme.

Uses:
It is used in the treatment of Alzheimer's disease.

Trihexyphenidyl

Action:
It belongs to Anti-Muscarinic Class.

Uses:It is used in the symptomatic treatment of Parkinson's disease.

Tolcapone

Action:
It caused inhibition of the enzyme Catechol-O-Methyl-Transferase (COMT) which results in the degradation of the dopamine.

Uses:
Tolcapone is used alongwith levodopa in the treatment of Parkinson's disease.

Selegiline

Mechanism of Action:
It selectively inhibits Monoamine Oxidase-B which causes the metabolism of dopamine and phenylethylamine.

Action:
It enhances and prolongs the Anti-Parkinsonian effects of levodopa but alone it is not of much benefit.

Uses:
It is used in the early stages of Parkinson's disease. It can also be used in Senile Dementia and depression.

Rotigotine

Action:
It is a dopamine agonist.

Uses:
It is used in the treatment of Parkinson's disease.

Dosage form:
It is available in the form of Transdermal Patches.

Ropinirole

It is available in the salt form of Ropinirole Hydrochloride.

Action:
It is a dopamine agonist.

Uses:
It is used in the treatment of Parkinson's disease.

Rasagiline

Action:
It is an irreversible inhibitor of Monoamine oxidase.

Uses:It is used either alone or with some other medications in the management of Parkinson's disease.

Procyclidine

It is available in the salt form of Procyclidine Hydrochloride.

Action:
It is an anticholinergic drug.
Uses:
It is helpful in the treatment of tremors in Parkinson's disease. It is also helpful in acute dystonia.

Pramipexole

Action:
It is a dopamine agonist.

Uses:It is used in early stages in the treatment of Parkinson's disease.

Levodopa

It is a levorotatory form of dopa i.e. L-dopa. It is a naturally occuring amino acid in certain foods and herbs.

Action:
It is converted into dopamine in the brain and body with the help of the enzyme dopa decarboxylase .

Uses:
It is used in the treatment of Parkinson's disease.

Entacapone

It is an anti-Parkinsonian drug.

Action:
It acts as Catechol-O-Methyl Transferase (COMT) inhibitor and helping levodopa to reach the brain easily by reducing its biotransformation.
It works effectively if taken alongwith levodopa and carbidopa i.e. combination of levodopa, carbidopa and entacapone (LCE). It has also been found that this combination did not increase motor complications.

Uses:
It is used in the treatment of Parkinson's disease. It has been found that prolonged treatment with entacapone results in enhanced response to levodopa in Patients of Parkinson's disease.

References:
Hauser, R. A.; Panniset, M.; 2008. Double-blind trial of levodopa/carbidopa/entacapone versus levodopa/carbidopa in early Parkinson's disease. Movement disorders, Vol. 24, No. 4, Pages 541-550.

Rinne, U. K., Larson, J. P. et al. 1998. Entacapone enhances the response to levodopa in parkinsonian patients with motor fluctuations. Neurology, Vol. 51, No. 5. Pages. 1309-1314.

Carbidopa

Action:
It causes inhibition of the peripheral metabolism of levodpa results in helping levodopa to reach the brain easily.

Uses:
It is used in combination with levodopa for the patients of Parkinson's disease.

Bromocriptine

It is available in the salt form of Bromocriptine Mesylate.

Action:
It is a dopamine agonist.
Uses:
It is used in the treatment of Parkinson's disease. It is also used in the treatment of Pituatory tumors, type 2 diabetes and neuroleptic malignant syndrome.

Biperiden

It is available in the salt form of Biperiden Hydrochloride or Biperiden lactate.

Action:
It possesses Anti-cholinergic properties.

Uses:
It is used in the management of Parkinson's disease.

Benztropine

It is available in the form of Benztropine Mesylate.

Action:
It possesses both Anti-cholinergic as well as Anti-histaminic properties. Its anti-cholinergic property is mainly important in the control of Parkinson's disease.
Uses:
It is used in the treatment of Parkinson's Disease.

Apomorphine

It is a derivative of morphine but is less active and work as a dopaminergic agonist.

Mechanism of Action:
It causes an increase in the dopamine amount in brain.
Uses:
It is used as an emetic and in little doses can also be used as sedative. It is also used as an Anti-parkinsonian agent.

Amantadine

It is used in the form of Amantadine Hydrochloride.

Mechanism of Action:
It helps in the treatment of Parkinson's disease by increasing the amount of dopamine in brain.

Uses:
It is an Anti-viral drug, used in the symptomatic or prophylactic treatment of Influenze-A, and is also used in the treatment of Parkinson's Disease.
It may also help in reducing dyskinesias.

Adverse Effects:
It may cause seizures in elderly people when used in high doses.

Atenolol

Therapeutic uses:

1. Hypertension
2. Angina pectoris
3. Cardiac dysarrhythmias

Safe in patients with diabetes or peripheral vascular disease

β-adrenoceptor blockers

Most β-adrenoceptor blockers are reversible and competitive antagonists for β-receptors. β-adrenoceptor blockers are of two types:

Beneficial effects in angina:
1. Through its β-blocking effect, it decreases sympathetic activation (i.e. catecholamine induction) of heart, resulting in

These effects decrease oxygen requirement of the muscles of the heart at rest as well as during physical activity.
2. Reduced heart rate causes an elevated diastolic perfusion time that promotes myocardial perfusion.

Adverse effects in angina:
As the heart rate is decreased, it causes an increased end diastolic volume and promoted ejection time.
This results in increased myocardial oxygen requirement.

Uses of β-blockers:
1. They are useful in classic angina

2. They decrease blood pressure in hypertension
3. They are helpful in cardiac arrhythmias
4. They are helpful in glaucoma
5. They are also helpful in therapy of myocardial infarction
6. Prophylactically helpful for treating migraine headache
It is used synchronously with nitrates to lessen its unwanted effects. On the other hand, this combination is also helpful for promoting duration of exercise as well as tolerance.

Contraindications:
It is contraindicated in patients of:
1. Asthma
2. Peripheral vascular disease
3. Chronic obstructive pulmonary disease
4. Diabetes

Diltiazem

It is similar in action to verapamil.


Actions:
It:
1. relieves spasm of coronary artery
2. causes a decrease in the AV conduction
3. causes a decrease in the firing time of the sinus node pacemaker
4. decrease heart rate
5. cause a depressed blood pressure

Therapeutic uses:
It is used for
1. variant angina.
2. Atrial fibrillation/flutter
3. Raynaud’s syndrome

Pharmacokinetics:
It undergoes hepatic metabolism.

Verapamil

It is a diphenylalkylamine.

Action:
It causes a decrease in the AV conduction of the heart leading to decreased heart rate and demand for oxygen. It also causes a decrease in the firing time of the sinus node pacemaker.

It has more negative inotropic effect as compared to nifedipine but has weak vasodilation effect.

Verapamil may also produce local anesthetic action (due to less effective blockade of sodium channels).

Verapamil also cause inhibition of insulin release.

Pharmacokinetics:
The drug shows hepatic metabolism.

Administration:
Orally, Intravenously

Therapeutic uses:
It is used for supraventricular tachyarrhythmias.

Adverse effects:
Constipation

Contraindications:
It is contraindicated in:
1. Patients with already decreased cardiac function.
2. Patients with abnormalities of atrioventricular conduction.

Precautions:
It should be used with caution in patients with liver function abnormalities.
It should also be used with caution in patients taking digoxin as it may increase digoxin level.

Nifedipine

It is a dihydropyridine derivative.


Actions:
It causes vasodilation of the arteries. It may cause peripheral vasodilation resulting in the decrease of total peripheral vascular resistance, resulting in decline of blood pressure declining oxygen requirement of the heart muscles.

It rarely affects on cardiac conduction or heart rate.

It may also decrease insulin secretion.


Dosage and administration:
It is administered orally and is available as extended release tablets.

Pharmacokinetics:
It undergoes hepatic metabolism and the metabolites (metabolism products) are excreted in urine and feces.

Therapeutic uses:
It is Useful in the treatment of variant angina (due to spontaneous coronary spasm).

Adverse effects:
Flushing, headache, hypotension, reflex tachycardia, peripheral edema, constipation,

Amlodipine

It does not affect the heart rate or cardiac output.

Structure:

Credit: Rxlist

Other names:

• Amlodipine Benzenesulfonate
• Amlodipine Besilate
• Amlodipine Besylate
• Amlodipine Free Base
• Amlodipino [Spanish]
• Amlodipinum [Latin]

Pharmacokinetics:
Its half life is 34 hours.

Therapeutic uses:
It is used for vasospastic chronic stable angina and hypertension.

Brand Names:

• Amlip (Venezuela)
• Amlocard (AWD (Germany))
• Amlodis (Eczacibasi (Turkey))
• Amlomed
• Amlopick
• Amvaz (Reddy (Malaysia))
• Coroval (Sandoz (Argentina))
• Lipinox  (Commonly misspelled Lipinok, Lepenox,Lilinox,Lipinux)
• Norvasc (Pfizer)

Also available in the following brands:

• Azor (amlodipine + olmesartan)
• Caduet (amlodipine + atorvastatin)
• Coroval B (amlodipine + benazepril)
• Exforge (amlodipine + valsartan)
• Lotrel (amlodipine + benazepril)

 
References:
Amlodipine on http://www.drugbank.ca/drugs/DB00381  Updated on November 10, 2010. Accessed April 17, 2011.

Calcium

Role of calcium:

Calcium is one of the essential components for contraction of muscles. Calcium is also responsible for the excitation-secretion coupling in exocrine and endocrine glands.

Calcium channels:

Calcium got entry into cells through pores in the membrane. These particular pores are named as calcium channels.

Types of calcium channels:

Action of calcium:

The calcium influx is elevated in ischemia as a result of membrane depolarization that is caused by reduced oxygen supply. This depolarization is voltage operated and is done by L- type channels. This increase results in the rise of activity of many ATP-consuming enzymes resulting in the reduction of energy stores. This leads in increase of ischemic effects.

Sometimes channels are opened by receptors for neurotransmitters and therefore this activation is referred to as receptor operated.

Mechanism of action of calcium entry blockers:

Calcium entry blockers get stick to receptors on voltage gated calcium channels resulting in blockage of these channels and saving tissues by preventing the entry of calcium into smooth muscle cells of the systemic arterial beds and muscle cells of coronary arteries (of the heart). Thus they reduce myocardial oxygen demand by saving ATP of muscles of the heart.

Some of the calcium entry blockers cause arteriolar dilatation; resulting from the decreased oxygen demand of the heart muscles, by affecting the heart directly i.e. causes the heart to beat slowly. They are, therefore, also working as vasodilators resulting in the decrease in smooth muscle tone and vascular resistance.

Actions:

Calcium entry blockers work better when the tissue is depolarized. At therapeutic doses, these agents affect on the resistance of vascular smooth muscle and the muscles of the heart.

They also decrease blood pressure.

They have negative chronotropic and inotropic effect resulting in less oxygen demand.

The prominent effect (anti-anginal) in angina caused by exercise and unstable angina is achieved by the reduction in cardiac afterload. On the other hand, vasospastic angina is relieved by dilatation of the coronary arteries and arterioles.

Calcium plays essential role in


1. contraction of muscles of the heart
2. regulating the firmness of the smooth muscles

Calcium get entry to the muscle cells through special channels namely voltage gated calcium channels. As a result, the release of calcium from the sarcoplasmic reticulum and mitochondria is initiated. This causes an additional elevation in the level of calcium in the fluid part of the cytoplasm (cytosol).
Therapeutic Uses:
They are also used in:
1. Systemic hypertension
2. Peripheral vascular disease
3. Hypertrophic subaortic stenosis
4. Stroke
5. Migraine
6. Suppression of atherogenesis

Adverse effects:
Hypotension, Headache, flushing, dizziness (These are caused by vasodilatory effects of calcium entry blockers).
Bradycardia (This is caused by less SA automaticity).
Heart block (This may be caused by reduced AV conduction).
Congestive heart failure (may be due to reduced contraction of the heart muscle).

Constipation (may be due to gentle excitation-contraction uncoupling in GI smooth muscle).

Calcium entry blockers

Much of the calcium entry blockers are dihydropyridines.

Clacium entry blockers include Amlodipine, Bepridil, Diltiazim, Felodipine, Isradipine, Nicardipine, Nifedipine, Nimodipine, Nisoldipine, Nitrendipine, Verapamil

Mechanism of action:

They get bind to receptors present on L-type calcium channels (voltage gated calcium channels) resulting in the blockage of calcium channels in the heart and in the smooth muscles of the coronary and peripheral vessels. This causes inhibition of calcium inflow to the cardiac and smooth muscle cells resulting in relaxation of muscles.

Actions:

Calcium channel blockers cause relaxation of the arterioles and veins but relaxation is more pronounced in arterioles than in the veins.

Calcium channel blockers causes dilatation of the coronary arterioles and coronary arteries and reduction of coronary artery spasm. This results in elevated oxygen supply to the muscles of the heart in patients with variant angina.

On the other hand, dilatation of the peripheral arterioles causes a decrease in total peripheral vascular resistance leading to decreased blood pressure. This affect is mainly caused by nifedipine. This causes a decrease in oxygen requirement of the muscles of the heart.

All of these factors are responsible for less oxygen requirement in patients with angina:

1. Reduced generation of impulses in SA node and reduced conduction in AV node

2. Reduced cardiac contractility and output

Verapamil and diltiazim show more pronounced effects on the heart.

Verapamil blocks release of insulin.

Verapamil blocks sodium channels less effectively, so that is why it has slight local anesthetic activity.

Pharmacokinetics:
They have a half life of about 2.5-8 hours, when used orally.

Therapeutic uses:
In hypertension when accompanied by angina, diabetes and/or asthma.

They are also used for angina pectoris, hypertrophic cardiomyopathy, migraine and atherosclerosis.

Verapamil is used to treat migraine, angina and supraventricular tachyarrhythmias.

Adverse effects:
They may cause dizziness, bradycardia, cardiac arrest, hypotension, nausea, constipation (in about 10% of patients), flushing and headache.

Contraindications:
These are contraindicated in patients with
1. cardiogenic shock
2. severe hypotension

Classification of Anti-Anginal Drugs

Classification according to differences in agents/groups:

Organic nitrites and nitrates:
Nitrites:
Amylnitrite,

Nitrates:
Erythrityl tetranitrate, Isosorbide dinitrate, isosorbide mononitrate, nitroglycerin, Pentaerythritol tetranitrate

β adrenoceptor blockers:
Nonselective β adrenoceptor blockers:
        Propranolol, Timolol, Nadolol
Selective β1 adrenoceptor blocker:
        Acebutolol, Atenolol, Metoprolol, Esmolol

Ca2+ entry blockers:
Amlodipine, Bepridil, Diltiazim, Felodipine, Isradipine, Nicardipine, Nifedipine, Nimodipine, Nisoldipine, Nitrendipine, Verapamil

Other vasodilator agents:
Dipyridamole, Nylidrin

Miscellaneous agents:
Camphotamide, Prenylamine

Plant products:
Papaverine

Classification according to types of angina pectoris:
Stable angina:
Nitroglycerin,

Variant angina:
Nitroglycerin, calcium entry blockers

Angina

It refers to a severe type of pain from any cause usually angina pectoris is considered.

Angina pectoris:
It is type of condition in which heart lacks blood supply resulting in severe constricting pains in the chest. The pain of angina pectoris often develops and spreads from the precordium of the heart to a shoulder (usually left) and down in the arm (of left side).

Cause of angina:
It may be due to ischemia of the myocardium usually produced as a result of coronary heart disease.

Types of angina:
It may be of different types:

1. Classical angina:
This is also referred to as angina of effort or exercise induced or stable angina or typical angina.
Symptoms:
It is marked by feeling of squeezed chest as well as burning in the chest.
Mechanism:
It may be due to blockage of the large coronary vessels leading to reduced coronary perfusion. This blockage may be caused by lipid deposits in the vessels.

2. Variant angina:

It is also called as vasospastic or prinzmetal’s angina. This often occurs at rest.

Mechanism:
1. It is caused by coronary artery spasm.
2. It also occurs as a result of less flow of blood to the muscles of the heart.

3. Unstable angina:

It occurs fewer than other types of angina and its cause is not among other causes of angina. It is in between stable angina and myocardial infarction. This often occurs at night in bed.

Stable Angina ---------- Unstable Angina ----------- Myocardial Infarction

Treatment of angina:

Angina is treated by any/both of the following mechanisms:
1. Promote perfusion of the muscles of the heart
2. Less metabolic demand of the muscles of the heart

Less requirement of oxygen in patients with angina is done by one of the following mechanisms:
1. Less generation of impulses in SA node
2. Reduced conduction velocity in AV node and Purkinje cells
3. Reduced contractions of the heart muscles
4. Reduced cardiac output.

Classification of Anti-Anginal Drugs

Transferrin

Transferrin: A protein in the serum which gets bound with the iron and helps in its transportation to the bone marrow.

Transcobalamin

Transcobalamin: A glycoprotein having the ability of binding to cobalamin.

Thymidylic acid

Thymidylic acid: It is an important part of DNA.

Thrombosis

Thrombosis: It denotes the blood clot formation within the blood vessel.

Thalasemia

Thalasemia: It is a hereditary type of anemia that is characterized by the disturbance in the synthesis of hemoglobin.

Succinyl-CoA

Succinyl-CoA: It is an intermediate product in the tricarboxylic acid cycle and is formed by the condensation of succinic acid and CoA.

Sickle-cell anemia

Sickle-cell anemia: A hereditary form of anemia.

Recombinant DNA technology

Recombinant DNA technology: It is the joining or recombining of two or more DNA pieces from different sources to yield a single (piece of) fragment.

Proximal

Proximal: Nearer part of the body.

Protoporphyrin

Protoporphyrin: A porphyrin acid that upon combination with iron forms iron containing proteins such as hemoglobin and cytochrome.

Porphyrin

Porphyrin: Compound in plants and animals consisted of four pyrrole rings that are linked with methylene group.

Polyglutamic acid

Polyglutamic acid: It is an acid made by the repeating molecules of glutamic acid residues in the normal peptide linkage.

Polycythemia vera

Polycythemia vera:
A chronic type of polycythemia without any known cause. Polyceythemia is the disease of excessive production of red blood cells in the body produced from the bone marrow.

Treatment for Polycythemia Vera:
Although allopathy is still unable to treat polycythemia vera but it works on the other conditions of the polycythemia vera like reduction of red blood cells and hemoglobin resulting in the reduction of the thickness of the blood.

Phlebotomy is normally done for the treatment of polycythemia vera. It is the procedure of removing some amount of blood from the body to reduce the amount of red blood cells.

Hydroxyurea and interferon alpha are also sometimes used in the treatment of polycythemia vera.

Herbal drugs for polycythemia:
Following most commonly occuring herbs may help in the treatment of polycythemia vera:

1. Garlic: as it may result in thinning of the blood.
2. Turmeric
3. Aloe vera

References:
Polycythemia Vera. http://www.nhlbi.nih.gov/health/dci/Diseases/poly/poly_treatments.html Accessed April 02, 2011.

Polycythemia

Polycythemia: Unusual increase in the red blood cells.

Pernicious anemia

Pernicious anemia: It is a serious type of anemia, usually in older age, characterized by the inability of the body to absorb vitamin B₁₂.

Neural

Neural: Relating to nerves.

Myelogenous

Myelogenous: Initiating from bone marrow.

Myelin

Myelin: It is a material composed of proteins and fats and is whitish in colour.

Mutase

Mutase: An enzyme involved in changing the arrangement of the certain molecules in a substance especially causing the movement of phosphate group from one atom of carbon to another.

Methylmalonyl-CoA

Methylmalonyl-CoA: Methylmalonyl-CoA has four atoms of carbon and is formed by the addition of carbon dioxide to propionyl coenzyme-A.