Usage
- Choline + Cyproheptadine is prescribed primarily to stimulate appetite and promote weight gain in patients with conditions like anorexia nervosa, inadequate dietary intake, and unintentional weight loss associated with chronic diseases like tuberculosis or HIV/AIDS. It is also prescribed for underweight children experiencing poor appetite due to various factors such as dietary issues, anemia, liver disease, or digestive disorders.
- Pharmacological classification: This combination medication falls under two categories: appetite stimulant (Cyproheptadine) and bile acid sequestrant (Choline).
- Mechanism of action: Choline citrate binds to bile acids in the intestine, promoting their excretion. This prompts the liver to utilize cholesterol to produce more bile acids, potentially lowering cholesterol levels. Cyproheptadine acts as an antihistamine and serotonin antagonist, particularly in the hypothalamus, the brain’s appetite control center. By blocking serotonin’s effect, it stimulates appetite.
Alternate Names
- While “Choline + Cyproheptadine” represents the generic name, there might be slight variations internationally.
- Brand names: The combination is marketed under various brand names which might vary regionally, such as Oraxin, Enzicap, Beterzyme, Zepup Orange. Periactin is the brand name for Cyproheptadine alone.
How It Works
- Pharmacodynamics: Choline enhances bile acid excretion, leading to increased cholesterol utilization by the liver. Cyproheptadine antagonizes serotonin receptors in the hypothalamus, stimulating appetite. It also has antihistaminic and anticholinergic properties.
- Pharmacokinetics: Cyproheptadine is well-absorbed orally and metabolized primarily in the liver, with renal excretion of metabolites. Choline is also absorbed orally and metabolized in the liver.
- Mode of action: Choline acts by binding to bile acids, facilitating their removal. Cyproheptadine exerts its appetite-stimulating effect by antagonizing serotonin receptors (specifically 5-HT2) in the hypothalamus.
- Receptor binding, enzyme inhibition, or neurotransmitter modulation: Cyproheptadine antagonizes serotonin (5-HT2), histamine (H1), and muscarinic receptors. Choline’s action is not mediated by receptor binding but rather by direct interaction with bile acids.
- Elimination pathways: Cyproheptadine is primarily metabolized in the liver and excreted in the urine as metabolites. Choline is also metabolized in the liver.
Dosage
Standard Dosage
Adults:
- The total daily dose should not exceed 0.5 mg/kg/day. The usual therapeutic range is 4-20 mg/day, divided into 2-3 doses. Some patients may require up to 32 mg/day.
- Oral administration (syrup, tablet).
Children:
- Dosage is based on age and weight. For children 2-6 years, the typical starting dose is 2 mg two or three times daily, not to exceed 12 mg/day. For children 7-14 years, the usual dose is 4 mg two or three times a day, not to exceed 16 mg/day.
- Oral administration (syrup, drops).
Special Cases:
- Elderly Patients: Start with lower doses (e.g., 4 mg twice daily) due to potential age-related decline in metabolic function and increased sensitivity to side effects.
- Patients with Renal Impairment: Reduce dosage and closely monitor for side effects as drug elimination might be decreased.
- Patients with Hepatic Dysfunction: Dose adjustment might be necessary due to decreased metabolism.
- Patients with Comorbid Conditions: Caution should be exercised in patients with glaucoma, prostatic hypertrophy, cardiovascular disease, hypertension, asthma, hyperthyroidism, or urinary retention issues.
Clinical Use Cases
- Dosing for specific clinical use cases like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations is not specifically established for this combination medication. Dosage adjustments in those cases are often extrapolated from standard and special case recommendations and rely on clinical judgment.
Dosage Adjustments
- Dosage adjustments should be made based on patient-specific factors such as renal/hepatic function, age, weight, concurrent medications, and response to therapy. Genetic polymorphisms affecting drug metabolism are not yet well established for this combination.
Side Effects
Common Side Effects
- Drowsiness
- Dizziness
- Dry mouth
- Blurred vision
- Constipation
Rare but Serious Side Effects
- Seizures
- Mental/mood changes (confusion, hallucinations, restlessness)
- Difficulty urinating
- Fast/irregular heartbeat
Long-Term Effects
- Chronic complications from prolonged use are not extensively documented, however continued monitoring of liver function, weight and appetite are advisable.
Adverse Drug Reactions (ADR)
- Serious allergic reactions (rash, itching/swelling, severe dizziness, trouble breathing)
Contraindications
- Hypersensitivity to cyproheptadine or choline.
- Newborn or premature infants.
- Nursing mothers.
- Narrow-angle glaucoma.
- Stenosing peptic ulcer, pyloroduodenal obstruction.
- Symptomatic prostatic hypertrophy.
- Bladder neck obstruction.
- Concomitant monoamine oxidase inhibitor (MAOI) therapy.
Drug Interactions
- CNS depressants (alcohol, sedatives, hypnotics): Additive CNS depression, increased drowsiness.
- MAOIs: Prolonged and intensified anticholinergic effects.
- Antihistamines: Additive anticholinergic effects.
- Certain antidepressants (e.g., SSRIs): Potential for serotonin syndrome.
- Anticonvulsants: Possible interaction, monitoring recommended.
- Narcotic analgesics: Additive CNS depression.
- Antipsychotics: Increased risk of anticholinergic effects.
Pregnancy and Breastfeeding
- Pregnancy: FDA Pregnancy Category B. Use only if clearly needed, benefits outweigh risks.
- Breastfeeding: Contraindicated. Cyproheptadine is excreted in breast milk and may suppress lactation.
Drug Profile Summary
- Mechanism of Action: Cyproheptadine: Serotonin antagonist in the hypothalamus; Tricholine citrate: Bile acid sequestrant.
- Side Effects: Drowsiness, dizziness, dry mouth, constipation, blurred vision.
- Contraindications: Hypersensitivity, newborns/prematures, nursing mothers, glaucoma, certain GI/GU obstructions, MAOI therapy.
- Drug Interactions: CNS depressants, MAOIs, antihistamines, certain antidepressants, anticonvulsants, narcotic analgesics, antipsychotics.
- Pregnancy & Breastfeeding: Pregnancy: Category B, use with caution; Breastfeeding: Contraindicated.
- Dosage: Adults: 4-32 mg/day; Children: 2-16 mg/day based on age; Adjust for renal/hepatic impairment.
- Monitoring Parameters: Appetite, weight, liver function tests, adverse effects.
Popular Combinations
- Commonly used with anti-tubercular and antiretroviral therapies to counteract weight loss associated with these conditions.
Precautions
- General Precautions: Evaluate for allergies, pre-existing medical conditions, and potential drug interactions before initiating therapy.
- Specific Populations: Pregnant Women: Use only if benefits outweigh risks. Breastfeeding Mothers: Avoid use. Children & Elderly: Adjust dosage and monitor closely.
- Lifestyle Considerations: Avoid alcohol, as it can exacerbate drowsiness. Advise against driving or operating machinery until effects are known.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Choline + Cyproheptadine?
A: Adults: 4-20 mg/day (up to 32 mg/day in some cases), divided into 2-3 doses. Children: 2-16 mg/day based on age and weight. Elderly: Start with a lower dose (e.g., 4 mg twice daily). Adjust for renal/hepatic impairment.
Q2: What are the primary uses of this medication?
A: Primarily used to stimulate appetite and promote weight gain in anorexia nervosa, underweight children, and weight loss associated with chronic illnesses.
Q3: What are the common side effects?
A: Drowsiness, dizziness, dry mouth, constipation, blurred vision.
Q4: Is this medication safe during pregnancy and breastfeeding?
A: Pregnancy: Category B; use with caution if benefits outweigh risks. Breastfeeding: Contraindicated.
Q5: What are the serious side effects to watch out for?
A: Seizures, mental/mood changes, difficulty urinating, fast/irregular heartbeat, allergic reactions.
Q6: What are the contraindications for this drug?
A: Hypersensitivity, newborns/prematures, nursing mothers, glaucoma, certain GI/GU obstructions, MAOI therapy.
Q7: Are there any specific drug interactions I should be aware of?
A: Yes, interactions can occur with CNS depressants, MAOIs, antihistamines, certain antidepressants, anticonvulsants, narcotic analgesics, and antipsychotics.
Q8: How does Choline contribute to this combination?
A: Choline acts as a bile acid sequestrant, promoting bile acid excretion and potentially lowering cholesterol levels.
Q9: Can this medication be used in elderly patients?
A: Yes, but with caution and at lower doses due to increased sensitivity to side effects.
Q10: What should patients be advised regarding lifestyle while on this medication?
A: Avoid alcohol and activities requiring alertness (driving, operating machinery) until the drug’s effects are known.
