ISINOR PLUS 6.2gm

Indications

• Severe infections caused by gram-negative bacteria
• Complicated urinary tract infections
• Bacterial sepsis
• Endocarditis caused by susceptible organisms

Dosage

Children: Dosing in children is also weight-based and varies by indication. Refer to the BNF for Children for specific dosing recommendations.

Adults: Dosage varies significantly based on the infection severity and type, renal function, and the specific bacterial susceptibility. Refer to clinical guidelines or the BNF for precise dosing.

Mechanism of action

Gram works by inhibiting bacterial protein synthesis. It binds to the 30S ribosomal subunit of the bacteria, causing misreading of the mRNA and ultimately preventing the synthesis of essential proteins necessary for bacterial growth and replication.

Pharmacodynamics

The pharmacodynamics of Gram include its bactericidal activity against susceptible bacteria. The drug shows concentration-dependent killing, meaning that higher drug concentrations correlate with greater bactericidal effects. The post-antibiotic effect is noted, where bacterial growth is inhibited even after the drug concentration falls below the minimum inhibitory concentration (MIC).

Pharmacokinetics

Gram is usually administered parenterally (intravenously or intramuscularly), and its absorption can vary based on the route of administration. It is distributed widely in body fluids and tissues, although it does not penetrate well into the central nervous system. The drug is primarily eliminated through the kidneys, and its half-life may be prolonged in patients with renal impairment. Monitoring of drug levels may be necessary to avoid toxicity.

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
• Allergic reactions
• Rash
• Renal dysfunction

Precautions

• Use with caution in patients with renal impairment
• Monitor renal function during therapy
• Assess for potential allergic reactions

Pregnancy

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

Breast-feeding

Use with caution, as it may be excreted in breast milk. Consult with a healthcare provider.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Indications

• Trypanosomiasis in cattle
• Prevention of African sleeping sickness in livestock

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations.

Adults: Refer to the BNF for specific dosing guidelines as it varies based on the condition and species treated.

Mechanism of action

Isometamidium acts by intercalating into the DNA of the parasite, disrupting replication and transcription processes. This impairs the synthesis of essential proteins and nucleic acids, leading to the death of the trypanosome.

Pharmacodynamics

The pharmacodynamics of isometamidium involve its selective toxicity to trypanosomes, which are more susceptible to its effects compared to mammalian cells. The drug's high affinity for the DNA of the parasites ensures that it efficiently inhibits their growth and replication. The efficacy of isometamidium is influenced by factors such as the strain of the trypanosome and the pharmacokinetic profile of the drug.

Pharmacokinetics

Isometamidium is administered parenterally, and it exhibits a relatively long half-life, allowing for sustained therapeutic levels in the bloodstream. The drug is distributed widely in body tissues, including the liver and kidney, where it can exert its effects against the parasites. It is metabolized in the liver and excreted primarily through urine, although specific metabolic pathways remain to be fully elucidated.

Pregnancy

Isometamidium should only be used if the potential benefit justifies the potential risk to the fetus. Consult relevant guidelines for use during pregnancy.

Breast-feeding

The effects on breastfeeding infants are unknown. Caution is advised when administering to nursing mothers.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Indications

• Pain relief
• Fever reduction
• Ear pain
• Testing drug metabolism

Dosage

Children: Refer to the BNF for Children for specific dosing guidance.

Adults: Refer to the BNF for specific dosing guidance.

Mechanism of action

Phenazone acts primarily in the central nervous system (CNS), increasing the pain threshold through the inhibition of cyclooxygenase enzymes, specifically COX-1, COX-2, and COX-3. This inhibition disrupts the synthesis of prostaglandins, which are mediators of pain and inflammation.

Pharmacodynamics

As an analgesic and antipyretic, phenazone serves to alleviate pain and reduce fever. It is frequently employed in pharmacological studies to assess the impact of other drugs or disease states on hepatic drug-metabolizing enzymes, demonstrating its importance in understanding drug interactions and metabolism.

Pharmacokinetics

Phenazone is absorbed well when administered orally. Its distribution in the body is extensive, and it is metabolized primarily in the liver, where it undergoes oxidation. The drug is excreted mainly through the kidneys. The elimination half-life can vary among individuals based on metabolic factors and liver function, necessitating caution in patients with hepatic impairment.

Adverse effects

• Nausea
• Vomiting
• Allergic reactions
• Skin rash
• Dizziness

Precautions

• Use with caution in patients with liver disease
• Monitor for signs of hypersensitivity

Pregnancy

Phenazone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether phenazone is excreted in human milk. Caution should be exercised when administering to a nursing mother.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Oral tablets
• Ear drops

Mechanism of action

Antipyrine is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1, COX-2, and COX-3 enzymes involved in prostaglandin (PG) synthesis.

Pharmacodynamics

Antipyrine is an analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29)