Rhodogil

Uses

Acne vulgaris, Cryptosporidiosis, Protozoal infections, Susceptible infections, Toxoplasmosis

Rhodogil is also used to associated treatment for these conditions: Bacterial Infections

How Rhodogil works

The mechanism of action of macrolides has been a matter of controversy for some time. Spiramycin, a 16-membered macrolide, inhibits translocation by binding to bacterial 50S ribosomal subunits with an apparent 1 : 1 stoichiometry. This antibiotic is a potent inhibitor of the binding to the ribosome of both donor and acceptor substrates. The primary mechanism of action is done by stimulation of dissociation of peptidyl-tRNA from ribosomes during translocation.I

Dosage

Rhodogil dosage

Intravenous-

Toxoplasmosis, Cryptosporidiosis, Protozoal infections, Susceptible infections:

• Adult: 1.5 million units by slow infusion every 8 hr, may double the dose in severe infections.

Oral-Cryptosporidiosis, Protozoal infections, Susceptible infections, Toxoplasmosis:

• Adult: 6-9 million units/day in 2-3 divided doses, increased to 15 million units/day, given in divided doses for severe infections.
• Child and neonates: Chemoprophylaxis of congenital toxoplasmosis: 50 mg/kg bid.

May be taken with or without food.

Side Effects

Nausea, vomiting, abdominal pain, diarrhoea; urticaria, pruritus, macular rashes. Transient paraesthesia may occur.

Toxicity

Cardiac toxicity, specifically QT prolongation (irregular heartbeat; recurrent fainting).
Cholestatic hepatitis (abdominal pain; nausea; vomiting; yellow eyes or skin).
Gastrointestinal toxicity, specifically acute colitis (abdominal pain and tenderness; bloody stools; fever).
Intestinal injury (abdominal pain and tenderness). Ulcerated esophagitis (chest pain; heartburn).

Precaution

Hepatic impairment; pregnancy and lactation. Monitor liver function. History of arrhythmias or predisposition to QT interval prolongation.

Interaction

Decreases carbidopa absorption and levodopa concentrations. Increased risk of ventricular arrhythmias when used with astemizole, cisapride and terfenadine. Risk of acute dystonia when used with fluphenazine

Volume of Distribution

The tissue distribution of spiramycin is extensive. The volume of distribution is in excess of 300 L, and concentrations achieved in bone, muscle, respiratory tract and saliva exceed those found in serum. Spiramycin showed high concentrations in tissues such as: lungs, bronchi, tonsils, and sinuses.

Elimination Route

The extent of absorption of Spiramycin was shown to be incomplete. Oral bioavailability ranges from 30-39%. Spiramycin has slower rate of absorption than Erythromycin. It has a high pKa (7.9) which could be a result of high degree of ionization in acidic medium of the stomach.

Half Life

Intravenous: Young persons (18 to 32 years of age): Approximately 4.5 to 6.2 hours. Elderly persons (73 to 85 years of age): Approximately 9.8 to 13.5 hours.

Oral: 5.5-8 hours, Rectal in children: 8 hours

Clearance

80% of the administered dose excreted in the bile, which makes the fecal-biliary route is the most important route of elimination. Enterohepatic recycling could also occur. Only 4 to 14% of an administered dose is eliminated through renal-urinary excretion route.

Elimination Route

Fecal-biliary route is the primary route of elimination. The secondary route is renal-urinary route.

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

Hypersensitivity.

Innovators Monograph

You find simplified version here Rhodogil