What Is Cyproheptadine?

Cyproheptadine is an anti-allergic drug that counteracts the effects of histamine on blood vessels and bronchial smooth muscles in the body, thereby eliminating allergic symptoms. Cyproheptadine can be used for allergic reactions such as urticaria, eczema, allergic and contact dermatitis, and pruritus.

Chinese name: Cyproheptadine
Foreign name: Cyproheptadine

Types of: drug
Function: anti-allergy

Brief introduction of cyproheptadine compounds

Cyproheptadine Basic Information

Cyproheptadine

Chinese name: sound heptidine

Chinese alias: cyproheptadine hydrochloride; ethylbenzene cycloheptimidine; antigan

English name: cyproheptadine hydrochloride sesquihydrate

English alias: Cyproheptadine hydrochloride; Cyproheptadine hydrochloride sesquihydrate; Piperidine (4- (5H-dibenzo [a, d] cyclohepten-5-ylidene) -1-methyl; 4- (5H-Dibenzo [a, d] cyclohepten-5-ylidene ) -1-methyl-piperidine hydrochloride hydrate; Antegan; Cipractin; Nuran; Peritol; Vimicon

CAS number: 41354-29-4

Molecular formula: C ₂₁ H ₂₄ ClNO

Molecular weight: 341.87400

Exact mass: 341.15500

PSA: 12.4000

LogP: 5.37350

Physical and chemical properties of cyproheptadine

Appearance and properties: white or light yellow crystalline powder, odorless and slightly bitter. 113 ° C melting point. The hydrochloride salt is slightly soluble in water, ethanol, chloroform, methanol, and almost insoluble in ether.

Melting point: 165 ° C (dec.) (Lit.)

Boiling point: 440.1ºC at 760 mmHg

Flash point: 194.5ºC

Cyproheptadine Safety Information

Symbol: GHS06

Signal Word: Danger

Hazard statement: H301; H315; H319; H335

Cautionary statements: P261; P301 + P310; P305 + P351 + P338

Dangerous Goods Transport Code: UN 2811 6.1 / PG 3

WGK Germany: 3

Danger category code: R22; R36 / 37/38

Safety instructions: S26-S36

RTECS number: TM7050000

Dangerous goods mark: Xn ^[1]

Use of cyproheptadine

New anticoagulant and antiallergic drugs. It can be used for allergic reactions such as urticaria, eczema, allergic and contact dermatitis, itching of the skin ^[1] .

Cyproheptadine drug description

Cyproheptadine Classification

Antiallergic Drugs> Antihistamines

Cyproheptadine dosage form

1. Tablets: 2mg, 4mg each.

2. Cream: 0.5% (hydrochloride).

Cyproheptadine pharmacological effects

Its H1 receptor antagonism is stronger than that of chlorpheniramine and promethazine, and it has a strong anti-serotonin effect and a mild anti-choline, anti-depression and central sedation effect. In addition, it also lowers blood sugar and increases appetite. Role. Its hypoglycemic effect may be through antihistamine and anti-serotonin, inhibiting growth hormone and corticotropin secretion from the pituitary gland, reducing both to increase insulin secretion, and its appetite-promoting effect may be due to inhibition of hypothalamic satiety. To. Its molecular structure is very similar to that of ketotifen, so cyproheptadine also has a certain mast cell and basophil cell membrane protection or mediator effect. In addition, it has an appetite stimulating effect ^[2] .

Cyproheptadine pharmacokinetics

Cyproheptadine is absorbed by the gastrointestinal mucosa after oral administration and takes effect within about 30 to 60 minutes. The peak drug concentration is reached in 2 to 3 hours, and the therapeutic effect can be maintained for 6 to 8 hours. Cyproheptadine is widely distributed and can cross the blood-cerebrospinal fluid barrier. Metabolism in the liver for the first time, oral 4mgC labeled cyproheptadine, 2% to 20% are excreted by feces, of which the original drug is 34%, more than 40% is excreted by the urine, the metabolites in the urine are glucuronic acid-bound quaternary ammonium Salt cyproheptadine. Cyproheptadine is also excreted through sweat, and a portion of breast milk is secreted by breastfeeding women. Medications for pregnant women can enter the fetus via cord blood, so women in early pregnancy should not take medication for a long time. Elimination slows down when renal insufficiency.

Cyproheptadine indication

Can be used for urticaria, eczema, allergic and contact dermatitis, itching of the skin, etc., with good curative effect. It can also be used for rhinitis, migraine, bronchial asthma, etc. It also has a certain effect on Cushing's disease and acromegaly. For Nelson syndrome (Nelson syndrome), anorexia nervosa, various allergic diseases, etc. In recent years, it has been reported that cyproheptadine has achieved good results in the treatment of acanthosis nigricans. It is mainly used for urticaria, eczema, allergic and contact dermatitis, such as eyelid contact dermatitis and allergic conjunctivitis.

Cyproheptadine contraindications

Glaucoma, prostatic hypertrophy, urinary retention, pyloric obstruction, peptic ulcer, and pregnant women, breastfeeding women, premature infants, and newborns are contraindicated.

Cyproheptadine dosage

oral. Adults: 4 to 20 mg daily, divided into 3 to 4 times. Children: 2 to 6 years old 2 mg each time, 2 to 3 times a day; 7 to 14 years old 4 mg each time, 2 to 3 times a day.

Cyproheptadine precautions

1. Avoid in patients with glaucoma.

2. Urinary retention, gastrointestinal ulcer, and pyloric obstruction should not be used in patients.

3. Do not use this product for premature delivery and newborns.

4. Avoid alcoholic beverages when taking medicine.

5. Those who are allergic to this product are prohibited.

6, the elderly and children under the age of two with caution.

7, driving machine, car, boat, engaged in aerial work, mechanical operators are prohibited during work.

8. Please consult a physician or pharmacist for the dosage of children.

9. Disable when the characteristics of this product change

10. Seek medical attention immediately if overdose or serious adverse reactions occur.

11. Children must be used under adult supervision.

12. Please keep this medicine out of the reach of children.

Cyproheptadine drug interactions

1. The combination of cyproheptadine and thyrotropin-releasing hormone may increase serum amylase and prolactin and affect the diagnosis.

2. The combination of cyproheptadine and monoamine oxidase inhibitor phenelzine can lead to the enhanced effect and toxicity of cyproheptadine, so the two should not be used in combination. In addition, cyproheptadine and other monoamine oxidase inhibitors (such as tranylcypromine, isocarbohydrazine, pagiline, phenethylhydrazine, etc.) and procarbazine, furazolidone, etc., which have monoamine oxidase inhibition Similar interactions can occur between them.

3. Central inhibitors can enhance central inhibitory effect when combined with cyproheptadine.

4. Cyproheptadine can reduce the analgesic effect of morphine.

5. The combination of cyproheptadine and atropine or other atropine drugs can increase atropine-like side effects, such as increasing symptoms of urinary retention, constipation, and dry mouth.

6. The combination of cyproheptadine and sutopril will increase the risk of ventricular arrhythmias, especially the tip twist caused by the addition of electrophysiological effects.

7. Valerian can enhance the effect of cyproheptadine.

8. Cyproheptadine has an anticholinergic effect (atropine-like effect), which can reduce the mitigating effect of cholinesterase drugs (such as ammonium chloride, neostigmine, dimemonium bromide, and eicosinate). . Sometimes it affects the treatment of glaucoma.

9. The combination of cyproheptadine with catecholamines can inhibit the uptake of catecholamines by neurons and increase the amount of free catecholamines. When combined, it can enhance the cardiovascular effects of catecholamines such as epinephrine and norepinephrine.

10. The combination of phenytoin sodium, primidone, ethanol and cyproheptadine can enhance each other. And combined with phenobarbital can mutually weaken their respective effects. If cyproheptadine is used in combination with nitrate drugs (such as nitroglycerin, pentaerythritol, etc.), it can enhance the effect of cyproheptadine or prolong its action time.

11. Combined with glucocorticoids can reduce the effect of glucocorticoids, while enhancing the anti-allergic effect of cyproheptadine.

12. Cyproheptadine can conceal the inner ear damage of aminoglycoside antibiotics such as streptomycin, neomycin, kanamycin, gentamicin, and nomomycin, making early toxicity symptoms difficult to find. This has irreversible consequences ^[2] .

Cyproheptadine adverse reactions

1. May have rash, photosensitivity, hypotension, tachycardia, extraperitoneal contraction, anaphylactic shock, hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia, fatigue, headache, insomnia, paresthesia , Convulsions, hallucinations, hysteria and other adverse reactions. Rare digestive disorders.

2. If long-term use of cyproheptadine can cause thick blood, it may also lead to increased appetite and weight gain. At high doses, insanity and ataxia can occur.

3. Cyproheptadine also has certain anticholinergic effects, causing dry mouth, bitter mouth, thick sputum, constipation, regulatory dysfunction, decreased lacrimal secretion, thick bronchial secretion, tachycardia, urinary retention, etc.

Cyproheptadine poisoning

Cyproheptadine has a strong antihistamine and serotonin effect, with mild anticholinergic, antidepressant, and central sedative effects; it also lowers blood sugar and stimulates appetite. It is mainly used for allergic diseases of various skin and mucous membranes. Orally absorbed, the plasma half-life is 16 hours, and the effect is maintained for 8 hours. Adults usually use 2 to 4 mg, 3 / d.

Clinical manifestations and diagnostic points

Common adverse reactions are drowsiness, dizziness, fatigue, nausea, excessive food, and weight gain.

treatment

The main points of treatment for cyproheptadine poisoning are:

Symptomatic treatment ^[3] .

Cyproheptadine Expert Reviews

Cyproheptadine has strong antihistamine and anti-serotonin effects, and also has anticholinergic and central sedative effects. Cyproheptadine has been reported to block calcium channels and inhibit aldosterone and adrenocorticotropic hormone secretion. Clinically used to relieve allergic reactions, including urticaria, eczema, allergic or contact dermatitis, pruritus, and allergic rhinitis. In addition, cyproheptadine has an appetite stimulating effect, and long-term use can increase weight. According to domestic reports, a hospital targeting human skin and blood vessels has both H1 and H2 histamine receptors, and combined use of H1 and H2 receptor antagonists, namely oral cyproheptadine and cimetidine, 3 times a day, each time separately For 2 mg and 400 mg, 43 patients with chronic urticaria were treated with 1 additional dose before bedtime for 1 month. The cure rate was 51% and the total effective rate was 95%, which is very different from the placebo double-blind controlled trial. The authors believe that combination medication is more effective and safer than any single medication. In another report, 50 cases of infants with asthma were treated with cyproheptadine at 0.25 mg / kg per day in two divided doses, while taking nifedipine at 0.5 to 1.9 mg / kg per day in two or three divided doses. As a result, the onset of asthma can be controlled relatively quickly, and the elimination time of symptoms and signs can be significantly shortened. The effective rate is more than 90%. In another 100 patients with mental illness, oral clozapine showed a drooling adverse reaction, while maintaining the former dose, cyproheptadine was added 8 to 16 mg each time, 3 times a day for 10 consecutive days. Results 78 cases of drooling disappeared, 21 cases were significantly reduced, and 1 case was ineffective. Continuing treatment, with the exception of one case, 99 cases of drooling disappeared ^[2] .

New uses of cyproheptadine

Cyproheptadine mumps

Cyproheptadine hydrochloride tablets

It has been found that chlorpheniramine combined with cimetidine has a good effect in treating mumps, and it has been proven that the H1 antagonistic effect of cyproheptadine hydrochloride is more than 5 times stronger than that of chlorpheniramine. From this, cyproheptadine hydrochloride 4-12 mg / day (adjusted with age) and cimetidine 20 mg / (kg · day) were tried orally in divided doses for a total of 4-7 days. Results: Of the 9 cases treated, 8 cases were cured, and the cure rate was 88.89%. The average antipyretic time and parotid swelling time were significantly better than those taking ribavirin and isatis root plus Chinese medicine.

Cyproheptadine anorexia in children

Usage: Oral, 2 mg / time, 3 times / day, even for 10-15 days. Generally, it is effective after 1 to 5 days after treatment, and those who are ineffective for more than 5 days after treatment are often ineffective. Those who relapse after discontinuation of the drug are still effective. Another person used cyproheptadine to treat 64 cases of pediatric anorexia, the effective rate was 85.8%. Most scholars believe that cyproheptadine is only suitable for non-organic weight loss such as anorexia nervosa and consumption status of tuberculosis. It is not recommended for healthy children whose height and weight are below the standard.

Cyproheptadine bronchial asthma

Usage: Oral, 4 mg / day, 3 times / day, 10 days is a course of treatment. After 2 to 3 days of general medication, symptoms can be alleviated or significantly reduced, with a total effective rate of 97.5%, which is significantly better than the control group treated with prednisone and dexamethasone (total effective rate 87.5%).

Cyproheptadine asthmatic bronchitis in children

Usage: 0.25 mg / (kg · day), orally divided into 3 times, 5 days as a course of treatment. Should be added with antibiotics. Results: The apparent efficiency was 55.4%, and the total effective rate was 92.3%. On the second day of general treatment, the spasm, asthma, and wheezing were significantly improved, the diet increased, and the spirit improved. The curative effect was better than the control group treated with aminophylline and promethazine.

- Cyproheptadine amenorrhea-lactation syndrome

Usage: Oral, 16-24 mg / day. It was reported that 15 female patients were treated with cyproheptadine, and after 10 weeks, the blood prolactin test decreased, menstruation returned to normal, 7 cases of lactation decreased, and 2 cases of lactation stopped.

Cyproheptadine dumping syndrome

The disease occurs after partial gastrectomy, with gastrointestinal symptoms such as abdominal distension, nausea, vomiting, abdominal cramps, diarrhea, and neurovascular symptoms such as sweating, pale, and palpitations. Oral cyproheptadine can be taken orally 1 to 2 hours before a meal to obtain significant effects.

Cyproheptadine for migraine

Usage: Oral, 2 mg / times, 3 times / day, then increase 2 mg daily, gradually increase to 12-20 mg / day, 6 months as a course of treatment, and start one after 3 to 4 weeks after withdrawal Course of treatment. Generally effective within 2 weeks. Preventive medication can be effective 30 minutes after taking the medication.

Cyproheptadine hepatic pruritus

Patients with cholestatic hepatitis, biliary cirrhosis, and post-hepatic cirrhosis often have intolerable skin pruritus, which affects sleep and rehabilitation. Commonly used antiallergic agents are often difficult to work. Cyproheptadine was used to treat 8 patients with cholestatic hepatitis and severe pruritus. After taking hormones, chlorpheniramine and other ineffective patients, changed to cyproheptadine, 4 mg / time, 3 times / day, and warm water. Symptoms generally improved after 3 days of taking the drug, with a total effective rate of 87.5%.

Cyproheptadine vertigo

Usage: Oral, 12 mg / day, plus low molecular weight dextran 250 ml / day intravenous drip treatment, the effective rate is 88.5%, dizziness is relieved within 1 to 2 days of administration, and stopped in 3 to 5 days.