Cimetidine – Dose, ROA, MOA, PK, PD, Indications & More

Dose and Dosage:

  • The typical adult dose of cimetidine for gastroesophageal reflux disease (GERD) is 800-1600 mg per day, divided into multiple doses.
  • For peptic ulcer disease, the usual dose is 800 mg at bedtime or 300 mg four times a day with meals and at bedtime.
  • Dosage adjustments may be necessary based on individual patient response and other medical conditions.

Frequency:

  • Cimetidine is usually taken multiple times per day, as prescribed by a healthcare provider.

Route of Administration (ROA):

  • Cimetidine is typically administered orally in the form of tablets, capsules, or oral liquid solutions.

Mechanism of Action (MOA):

  • Cimetidine is a histamine H2-receptor antagonist that competitively inhibits histamine at the H2 receptors of the gastric parietal cells, thereby reducing gastric acid secretion.

Pharmacokinetics (PK):

  • Cimetidine is well absorbed after oral administration, with peak plasma concentrations reached within 1-3 hours.
  • It undergoes extensive hepatic metabolism, primarily by the cytochrome P450 enzyme system.
  • The elimination half-life is approximately 2 hours, with renal excretion of both unchanged drug and metabolites.

Pharmacodynamics (PD):

  • Cimetidine exerts its therapeutic effects by reducing gastric acid secretion, leading to decreased acidity in the stomach and relief of symptoms associated with GERD and peptic ulcer disease.

Pathophysiology:

  • Cimetidine acts on the histamine H2 receptors in the stomach, blocking the action of histamine, which normally stimulates acid secretion. By inhibiting acid production, cimetidine helps to alleviate symptoms associated with conditions such as GERD and peptic ulcers.

Indications:

  • Cimetidine is indicated for the treatment of active duodenal ulcers, benign gastric ulcers, GERD, erosive esophagitis, pathological hypersecretory conditions (e.g., Zollinger-Ellison syndrome), and as part of combination therapy for the prevention of stress ulcers.

Contraindications:

  • Hypersensitivity to cimetidine or any component of the formulation
  • Known hypersensitivity to other H2-receptor antagonists
  • Co-administration with drugs that require gastric pH-dependent absorption

Drug Interactions:

  • Cimetidine may interact with various medications, including anticoagulants, benzodiazepines, beta-blockers, phenytoin, theophylline, and tricyclic antidepressants, among others. It can affect the metabolism of these drugs by inhibiting cytochrome P450 enzymes.

Monitoring and Laboratory Tests:

  • Patients taking cimetidine may require periodic monitoring of liver function tests, particularly with long-term use or in individuals with pre-existing liver disease.
  • Monitoring for signs and symptoms of adverse effects, such as CNS effects, gynecomastia, or hematological abnormalities, may also be warranted during therapy.

Why is this medication prescribed?

Cimetidine is prescribed to treat conditions related to excessive stomach acid production, including:

  • Peptic ulcer disease
  • Gastroesophageal reflux disease (GERD)
  • Erosive esophagitis
  • Pathological hypersecretory conditions (e.g., Zollinger-Ellison syndrome)

How should this medicine be used?

  • Cimetidine is typically taken orally, usually multiple times per day.
  • Dosage and frequency depend on the specific condition being treated and individual patient factors.
  • It is essential to follow the dosing instructions provided by the healthcare provider.

Other uses for this medicine

Cimetidine may also be used off-label for other conditions, such as:

  • Treatment of heartburn
  • Prevention of stress ulcers in critically ill patients

However, the off-label use should only be done under the guidance of a healthcare professional.

What special precautions should I follow?

  • Inform your healthcare provider about any allergies, medical conditions, or medications you are currently taking.
  • Cimetidine may interact with various drugs, so inform your doctor about all prescription, over-the-counter, and herbal products you are using.
  • Follow your doctor’s instructions carefully, especially regarding dosage and frequency.

What special dietary instructions should I follow?

  • There are no specific dietary restrictions associated with cimetidine use.
  • However, avoiding foods and beverages that can exacerbate symptoms of GERD or peptic ulcers, such as spicy foods, caffeine, and alcohol, may be beneficial.

What should I do if I forget a dose?

  • If you miss a dose of cimetidine, take it as soon as you remember.
  • However, if it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule.
  • Do not take a double dose to make up for a missed one.

What side effects can this medication cause?

Common side effects of cimetidine may include:

  • Headache
  • Dizziness
  • Diarrhea
  • Nausea or vomiting
  • Constipation
  • Fatigue

Rare but serious side effects may include:

  • Allergic reactions
  • Changes in liver function
  • Blood disorders
  • Central nervous system effects

Report any unusual or severe side effects to your healthcare provider promptly.

What should I know about storage and disposal of this medication?

  • Store cimetidine tablets or capsules at room temperature, away from moisture and heat.
  • Keep the medication out of reach of children and pets.
  • Follow any specific storage instructions provided by your pharmacist.
  • Dispose of any unused medication properly, according to local regulations or guidelines.

In case of emergency/overdose

  • In case of overdose, contact your local poison control center or seek emergency medical attention immediately.
  • Symptoms of overdose may include confusion, hallucinations, rapid heartbeat, and difficulty breathing.