S-PYRIMAC TABLES (Each dispersible tablet contains Sultodoxine/ Pyramethane 500/125mg

Indications

• Treatment of acute malaria caused by Plasmodium falciparum
• Prophylaxis of malaria in areas where the disease is endemic
• Treatment of toxoplasmosis in combination with sulfadiazine

Dosage

Children: Refer to appropriate pediatric dosing guidelines in the BNF for Children as specific doses may vary based on age and weight.

Adults: Refer to established guidelines for specific dosing based on the clinical condition and severity of malaria. It is important to consult the BNF or a healthcare professional for the recommended dosage.

Mechanism of action

Pyramethamine acts as a selective inhibitor of dihydrofolate reductase (DHFR), an enzyme involved in the folate pathway. By inhibiting DHFR, pyramethamine disrupts the synthesis of tetrahydrofolate, a cofactor necessary for the production of nucleic acids and amino acids, thereby impairing the growth and multiplication of malaria parasites.

Pharmacodynamics

Pyramethamine exhibits a synergistic effect when used in combination with sulfonamides, as both act on the folate synthesis pathway but at different sites. This combination enhances the overall efficacy against Plasmodium species. The drug is effective against both the asexual and sexual forms of the malaria parasite, making it useful in both treatment and prophylaxis.

Pharmacokinetics

Pyramethamine is well absorbed from the gastrointestinal tract, with peak plasma concentrations typically occurring within 2 to 6 hours after oral administration. It is widely distributed throughout the body, including the central nervous system. The drug is metabolized predominantly in the liver and has a half-life ranging from 5 to 14 days. Renal excretion is the primary route of elimination, and dosage adjustments may be necessary in cases of renal impairment.

Contra-indications

• Hypersensitivity to pyramethane or any of its components
• Severe hepatic impairment
• Severe renal impairment

Adverse effects

• Drowsiness
• Dizziness
• Dry mouth
• Nausea
• Vomiting
• Hypotension
• Blurred vision

Interactions

• Increased sedation with central nervous system depressants
• Potential interaction with antihypertensive medications

Precautions

• Use with caution in patients with a history of substance abuse
• Monitor for signs of sedation
• Caution in elderly patients or those with comorbid conditions

Pregnancy

Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult with healthcare provider.

Breast-feeding

Use with caution during breastfeeding. Consult with healthcare provider to assess risks and benefits.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.

Formulations

• Oral tablets
• Syrup
• Injection

Indications

• Methicillin-resistant Staphylococcus aureus (MRSA) infections
• Pneumonia caused by resistant Gram-positive bacteria
• Skin and soft tissue infections
• Bacteremia or sepsis due to Gram-positive organisms

Dosage

Children: Refer to specific recommendations in the BNF for Children for appropriate dosing details.

Adults: Refer to specific recommendations in clinical guidelines or formularies for appropriate dosing details.

Mechanism of action

Ultodoxine exerts its antibacterial effects through the inhibition of protein synthesis in bacteria. It binds to the 23S rRNA of the 50S ribosomal subunit, preventing the formation of the ribosomal complex necessary for translation. This action effectively halts the production of essential proteins required for bacterial growth and replication.

Pharmacodynamics

The pharmacodynamics of ultodoxine involve its bacteriostatic activity against a broad spectrum of Gram-positive organisms. Its efficacy is influenced by the concentration of the drug at the site of infection and its ability to penetrate bacterial cells. Resistance to ultodoxine can develop through mutations that alter the drug's target site on the ribosome.

Pharmacokinetics

Ultodoxine is absorbed well after oral administration, with peak plasma concentrations occurring within a few hours. It has a large volume of distribution, allowing adequate tissue penetration, particularly in areas such as the lungs and skin. The drug is metabolized in the liver and excreted primarily in the urine. The half-life of ultodoxine is variable but typically ranges from 5 to 7 hours, necessitating appropriate dosing intervals to maintain therapeutic levels.

Pregnancy

Not enough data is available to determine safety during pregnancy. Consult healthcare provider.

Breast-feeding

Limited information is available on the excretion of ultodoxine in human milk. Caution is advised.

Storage

Store at room temperature, away from moisture and heat. Protect from light.