Tuesday, March 22, 2011

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.

Monday, March 21, 2011

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.