Cyproheptadine (Cyproheptadinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

H1-antihistamines

Serotonergic agents

Included in the formulation
  • Peritol®
    syrup inwards 
    EGIS ZAO Pharmaceutical Plant     Hungary
  • Peritol®
    pills inwards 
    EGIS ZAO Pharmaceutical Plant     Hungary
    • АТХ:

    R.06.A.X.02   Cyproheptadine

    Pharmacodynamics:

    Pharmacological action - antihistamine, antiallergic, antiserotonin.

    It blocks histamine H1-receptors. Reduces the body's response to histamine, prevents and alleviates the course of allergic reactions. Reduces the permeability of capillaries, prevents the development of edema of tissues. Has a pronounced antiserotonin, weak m-holinoliticheskoe and sedative effect. Reduces hypersecretion of somatotropin in acromegaly and ACTH release in Isenko-Cushing syndrome.

    In experimental studies, there was no mutagenic and teratogenic effect, effects on fertility.

    Pharmacokinetics:

    When ingested quickly and completely absorbed from the digestive tract. Maximum concentration is achieved during the first 2 hours, the therapeutic level in the plasma persists for 4-6 hours. It is evenly distributed in the body, penetrates into the central nervous system. Intensively metabolized (hydroxylation followed by the formation of conjugates with glucuronic acid) in the liver.After a single application in a dose of 4 mg (in the form of tablets or syrup), 2-20% is excreted by the intestine (of which 34% is unchanged) and at least 40% is excreted in the urine. With repeated daily use in doses of 12-20 mg (as a syrup), the unchanged form of the drug in the urine is not detected. The main metabolite found in urine is identified as a quaternary ammonium conjugate of cyproheptadine with glucuronic acid. With renal failure, the elimination slows down.

    Indications:

    Hives (acute, chronic and cold), pollinosis, serum sickness, year-round or seasonal allergic rhinitis, allergic conjunctivitis, angioedema; allergic reactions to taking medicinal and radiocontrast agents, blood transfusions, insect bites; skin diseases - itching dermatoses, contact dermatitis, toxicodermia, neurodermatitis, eczema; headache of vascular origin (migraine), vasomotor rhinitis; anorexia, cachexia (in the period of convalescence, with chronic diseases), complex therapy of chronic pancreatitis.

    ICD-10

    XII.L20-L30.L30.9   Dermatitis, unspecified

    XII.L20-L30.L23   Allergic contact dermatitis

    XII.L20-L30.L20   Atopic dermatitis

    XVIII.R50-R69.R63.0   Anorexia

    XII.L20-L30.L29   Itching

    X.J30-J39.J30   Vasomotor and allergic rhinitis

    XI.K80-K87.K86.1   Other chronic pancreatitis

    VII.H10-H13.H10.1   Acute atopic conjunctivitis

    VI.G40-G47.G43   Migraine

    XVIII.R50-R69.R51   Headache

    XVIII.R20-R23.R21   Rash and other nonspecific skin rashes

    XX.W50-W64.W57   Bite or sting with a non-toxic insect or other non-venous arthropod

    XIX.T80-T88.T80.6   Other serum reactions

    Contraindications:

    Hypersensitivity, zakratougolnaya glaucoma, benign prostatic hyperplasia, urinary retention, pyloroduodenal obstruction, stenosing peptic ulcer, predisposition to edema, simultaneous use with MAO inhibitors, pregnancy, breast-feeding, breast age (up to 6 months).

    Carefully:

    Caution is prescribed for children and elderly patients (hypersensitivity is possible), patients with a history of bronchial asthma, hyperthyroidism, increased intraocular pressure, arterial hypertension and other cardiovascular diseases.

    Pregnancy and lactation:

    Action category for the fetus by FDA - B. Adequate and well-controlled studies on humans have not been conducted. Do not apply.

    Penetrates into breast milk. The use is not recommended due to increased excitability in infants. Can inhibit lactation due to the presence of anticholinergic activity. For the duration of treatment, breastfeeding should be discontinued.

    Dosing and Administration:

    The first reception is recommended in the evening, after a meal (for the start of treatment is characterized by a sedative effect).

    Inside after eating. Adults - 4 mg 3 times a day; for the treatment of chronic urticaria - 2 mg 3 times a day; with an acute migraine attack - 4 mg once, in the absence of effect after 30 minutes - 4 mg more; for maintenance therapy - 4 mg 3 times a day; with anorexia - 12 mg in three divided doses; the maximum daily dose is 32 mg. The duration of treatment to increase body weight should not exceed 6 months. Children from 6 months to 2 years (with caution only in special cases) - up to 0.4 mg / kg per day for 3-4 weeks, 2-6 years - 6 mg per day, 6-14 years - 12 mg in day, with anorexia - up to 8 mg per day in 3 divided doses. The duration of treatment for anorexia and cachexia is not more than 3 months. Maximum daily doses in children 2-6 years - 8 mg, 6-14 years - 16 mg.

    Side effects:

    From the side nervous system and sense organs: weakness, sedation and drowsiness (often transient), anxiety, headache, dizziness, ataxia, visual hallucinations.

    From the side cardiovascular system and blood (hematopoiesis, hemostasis): hypotension, tachycardia, hemolytic anemia, leukopenia, agranulocytosis.

    From the side organs of the digestive tract: dry mouth, nausea, vomiting, diarrhea.

    Allergic reactions: rash, angioedema, hives, anaphylaxis, photosensitivity.

    Other: increase in body weight.

    Overdose:

    Symptoms: in children - mydriasis and the immobility of the pupils, hyperemia of the facial skin, hyperthermia, agitation, anxiety, hallucinations, ataxia, athetosis, convulsions, collapse, coma; in adults - retardation, depression, coma, or psychomotor agitation, convulsions; rarely - hyperthermia and hyperemia of the skin.

    Treatment: induction of vomiting, the appointment of activated charcoal inside, followed by gastric lavage; with the development of life-threatening symptoms from the side of the central nervous system or pronounced atropine-like effects - the introduction of a solution of physostigmine salicylate; by indications - vasoconstrictive and anticonvulsants, mechanical ventilation, and other resuscitation measures. Psychostimulants and analeptic agents are contraindicated.

    Interaction:

    Caffeine reduces the inhibitory effect of cyproheptadine on the CNS; additive effect can be observed with the joint application of cyproheptadine with ethyl alcohol and other substances that depress the central nervous system (sedatives, hypnotics, anxiolytics).

    Simultaneous use of cyproheptadine with other drugs that depress the central nervous system requires constant monitoring of the patient and withdrawal of the drug if necessary.

    Combined use of cyproheptadine with fluoxetine and other inhibitors of reverse neuronal seizure of serotonin leads to a decrease in the effectiveness of antidepressants.

    Contraindicated simultaneous use of cyproheptadine with MAO inhibitors. MAO inhibitors, as well as tricyclic antidepressants, can prolong and intensify the m-holin-blocking effect of cyproheptadine, and enhance the inhibitory effect on the CNS.

    Special instructions:

    During course treatment, you should not drink alcohol.

    It can be used together with narcotic analgesics, anxiolytics (under strict medical supervision) for complex preoperative preparation of patients, since cyproheptadine potentiates the effect of these drugs with simultaneous use and prevents the development of undesirable effects of histamine (arterial hypotension, bronchospasm), which is released as a result of traumatization of body tissues during surgery.

    Do not use during work drivers of vehicles and people whose profession is associated with increased concentration of attention, especially in the initial, individually defined period of treatment.

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