Usage
- This combination is primarily prescribed as an appetite stimulant to address conditions like anorexia, weight loss, and poor appetite in various clinical situations, including undernutrition, inadequate dietary intake, and as an adjunct therapy in conditions like tuberculosis and HIV/AIDS where weight gain is desired. It is also used in children experiencing insufficient growth and development due to poor nutritional intake.
- Pharmacological Classification: Cyproheptadine is an antihistamine with antiserotonergic properties, and Tricholine Citrate is a bile acid-binding agent with lipotropic effects. Therefore, this combination could be categorized as an appetite stimulant and a metabolic support medication.
- Mechanism of Action: Cyproheptadine primarily acts by blocking histamine and serotonin receptors in the hypothalamus, an area of the brain that regulates appetite. By antagonizing serotonin’s effect on appetite suppression, Cyproheptadine helps stimulate appetite. Tricholine Citrate enhances liver function and indirectly supports metabolism. It acts by binding to bile acids in the intestine, facilitating their excretion. This prompts the liver to produce more bile acids, utilizing cholesterol, potentially leading to a decrease in fat content.
Alternate Names
- No widely recognized alternate names exist for this specific combination. The individual components, Cyproheptadine and Tricholine Citrate, are the standard generic names used internationally.
- Brand Names: This combination is marketed under various brand names like Peptone Gold, Oraxin, Cyploc, and others. The specific brand name will vary depending on the manufacturer and the region.
How It Works
- Pharmacodynamics: Cyproheptadine exerts its effects primarily by acting as a histamine and serotonin antagonist. Its appetite-stimulating properties are attributed to its action on serotonin receptors in the hypothalamus. Tricholine Citrate supports liver function and metabolic processes by acting as a lipotropic agent, thus aiding in fat metabolism.
- Pharmacokinetics: Cyproheptadine is well-absorbed orally and is metabolized primarily in the liver, with excretion occurring mainly via the kidneys. Tricholine Citrate is also absorbed well orally and is metabolized to form choline, which plays various roles in metabolic pathways. Specific details on CYP enzyme involvement are not explicitly mentioned in the provided resources.
- Mode of Action: Cyproheptadine competes with histamine and serotonin at their receptor sites, effectively blocking their effects. It inhibits the appetite-suppressing action of serotonin in the hypothalamus. Tricholine Citrate acts by binding to bile acids, reducing their enterohepatic recirculation and increasing their fecal excretion.
- Elimination Pathways: Cyproheptadine is metabolized extensively in the liver, followed by renal excretion. Tricholine Citrate is metabolized to choline, which is further metabolized and excreted. Elimination is diminished in renal insufficiency and hepatic impairment.
Dosage
Standard Dosage
Adults:
- The typical adult dose is 4-20 mg/day of Cyproheptadine, often divided into 2-3 doses, with a maximum not exceeding 0.5 mg/kg/day. Combined with 275-825 mg of Tricholine Citrate, also typically divided into 2-3 doses.
Children:
- Dosage in children is weight or age-based and should be determined and supervised by a physician. Typical ranges are 0.25 mg/kg/day or 8 mg/m²/day of Cyproheptadine and 275-825 mg of Tricholine Citrate/ day.
- The usual dose for children 2-6 years old is 2 mg of Cyproheptadine two or three times a day, not exceeding 12 mg/day combined with 275 mg of Tricholine Citrate. For children 7-14 years old, it’s 4 mg two or three times a day, not exceeding 16 mg/day combined with 275-550 mg of Tricholine Citrate.
- Pediatric safety considerations include careful monitoring for side effects, especially drowsiness and anticholinergic effects. Safety and efficacy in children under 2 years old have not been established.
Special Cases:
- Elderly Patients: Due to potential increased sensitivity to anticholinergic effects, start with lower doses (e.g., 4 mg every 12 hours of Cyproheptadine) and monitor closely.
- Patients with Renal Impairment: Dose adjustments are necessary due to reduced clearance of Cyproheptadine. Closer monitoring is warranted.
- Patients with Hepatic Dysfunction: Use with caution. Dose adjustments may be necessary. Close monitoring is recommended.
- Patients with Comorbid Conditions: Pre-existing conditions like asthma, glaucoma, urinary retention, hypertension, or cardiovascular disease require careful consideration and potential dose adjustments.
Clinical Use Cases
- The provided sources primarily address its use in appetite stimulation. There’s no specific mention of its use in settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
- Dose modifications are essential based on patient-specific factors like age, renal/hepatic function, and co-existing medical conditions. Genetic polymorphisms affecting drug metabolism are not mentioned, however individual patient responses should be closely monitored.
Side Effects
Common Side Effects:
- Drowsiness, dizziness, dry mouth, blurred vision, constipation, nausea, confusion, and disturbed coordination.
Rare but Serious Side Effects:
- Allergic reactions (rash, hives, swelling), hallucinations, seizures, CNS depression, cardiovascular effects (hypotension, tachycardia, palpitations), and urinary retention.
Long-Term Effects:
- Long-term use may lead to chronic anticholinergic effects, tolerance to appetite stimulation, or potential liver/kidney dysfunction, although more data is needed.
Adverse Drug Reactions (ADR):
- Severe allergic reactions, serotonin syndrome, significant CNS depression, or cardiovascular effects.
Contraindications
- Hypersensitivity to Cyproheptadine or Tricholine Citrate; narrow-angle glaucoma; stenosing peptic ulcer; bladder neck obstruction; symptomatic prostatic hypertrophy; newborn or premature infants; nursing mothers; concomitant use of MAO inhibitors.
Drug Interactions
- MAO inhibitors: May potentiate anticholinergic effects.
- CNS depressants (alcohol, sedatives, hypnotics, tranquilizers): Additive sedative effects.
- Antihistamines: May increase drowsiness.
- Antidepressants (particularly MAOIs and some SSRIs): May enhance cyproheptadine’s effects or lead to serotonin syndrome.
- Anticholinergics: May potentiate anticholinergic effects.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Cyproheptadine is categorized as Pregnancy Category B, indicating that animal studies have not demonstrated fetal harm, but controlled studies in pregnant women are lacking. Its use during pregnancy should only be considered if the potential benefit outweighs the risk.
- Use during breastfeeding is not recommended, as it may pass into breast milk and cause infant drowsiness or other adverse effects. It can also affect prolactin levels which are essential for lactation.
Drug Profile Summary
- Mechanism of Action: Cyproheptadine: Histamine and serotonin antagonist. Tricholine Citrate: Bile acid-binding agent.
- Side Effects: Drowsiness, dizziness, dry mouth, blurred vision, constipation, confusion.
- Contraindications: Hypersensitivity, glaucoma, urinary retention, MAOI use.
- Drug Interactions: MAOIs, CNS depressants, anticholinergics.
- Pregnancy & Breastfeeding: Pregnancy Category B, not recommended during breastfeeding.
- Dosage: Adults: 4-20 mg/day; Children: Weight/age-based.
- Monitoring Parameters: Appetite, weight, liver function tests, mental status.
Popular Combinations
- Often used alone or with supplemental vitamins and minerals to address nutritional deficiencies. Combining it with other appetite stimulants might not be routine and may be under strict monitoring from healthcare professionals.
Precautions
- General Precautions: Assess for allergies, pre-existing medical conditions (especially glaucoma, urinary issues, and cardiovascular disease), and concomitant medications.
- Specific Populations: Use with caution in the elderly, patients with renal/hepatic impairment, and those with asthma or hypertension.
- Lifestyle Considerations: Advise patients against alcohol consumption while taking this medication, and caution regarding operating machinery due to potential drowsiness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Cyproheptadine + Tricholine Citrate?
A: The recommended dosage varies depending on the patient’s age, weight, and medical condition. Adults typically receive 4-20 mg/day of Cyproheptadine, often divided into 2-3 doses, with a maximum of 0.5 mg/kg/day combined with 275-825 mg of Tricholine Citrate. Children’s dosages are calculated based on their weight or body surface area.
Q2: What are the primary uses of this medication?
A: This combination is mainly used to stimulate appetite and promote weight gain in cases of anorexia, undernutrition, or as an adjunct therapy for conditions requiring weight gain (e.g., TB, HIV/AIDS).
Q3: What are the common side effects?
A: Common side effects include drowsiness, dizziness, dry mouth, blurred vision, constipation, nausea, confusion, and impaired coordination.
Q4: Is it safe to use during pregnancy and breastfeeding?
A: Cyproheptadine is Pregnancy Category B, but its use should only be considered if the potential benefit outweighs the potential risk. It is not recommended for use during breastfeeding.
Q5: Are there any specific contraindications?
A: Yes, contraindications include hypersensitivity, narrow-angle glaucoma, urinary retention issues, and concomitant use of MAO inhibitors.
Q6: What are the potential drug interactions I should be aware of?
A: Potentially interacting medications include MAOIs, CNS depressants, other antihistamines, antidepressants (especially MAOIs and SSRIs), and anticholinergic drugs.
Q7: How does Tricholine Citrate contribute to this combination?
A: Tricholine Citrate helps promote healthy liver function, supports metabolic processes, and might indirectly aid in weight gain.
Q8: Should I adjust the dosage for elderly patients?
A: Yes, elderly patients may require lower starting doses due to increased sensitivity to side effects.
Q9: Are there any dietary restrictions while taking this medication?
A: It is generally advisable to avoid alcohol while taking this medication as it can exacerbate drowsiness.
Q10: Can this medicine be used in children under 2 years old?
A: The safety and efficacy of this medicine in children younger than 2 years old have not been established. Therefore, it’s not typically recommended for this age group.
