Periactin 4 mg Tablets

Brand name

The trade name of the drug is Periactin. This is the registered name under which the drug is known in medical practice and is available in pharmacies.

International Nonproprietary Name (INN)

The international nonproprietary name is cyproheptadine. This name indicates the active active ingredient and is used in pharmacology to identify the drug internationally.

Form of release

Periactin is available in two main forms: tablets of 4 mg, packed in blisters of 20 or 30 pieces, and syrup with a concentration of 2 mg/5 ml, supplied in bottles of 100 ml or 200 ml with a measuring spoon. The tablets are round in shape and white in color, which simplifies their identification, and the syrup has a pleasant taste, which facilitates its use in children.

Composition

Active substance

The main active ingredient is cyproheptadine hydrochloride. One tablet contains 4 mg of cyproheptadine hydrochloride, and 5 ml of syrup contains 2 mg of this substance.

Auxiliary ingredients

The tablets include ingredients such as lactose monohydrate, microcrystalline cellulose, pregelatinized starch, magnesium stearate, which provide stability and ease of administration. The syrup contains sucrose, sorbitol, glycerin, citric acid, sodium benzoate (as a preservative) and flavoring to give it a pleasant taste and smell.

Pharmacologic Properties

Pharmacodynamics

Cyproheptadine, the active ingredient of Periactin, is a potent H1-histamine receptor antagonist and has the additional ability to block serotonin receptors (5-HT2). Its antihistamine action is aimed at inhibiting allergic reactions such as itching, tissue swelling, mucus hypersecretion and skin rashes by preventing histamine binding to the corresponding receptors. The antiserotonin effect plays a key role in appetite stimulation, as serotonin is involved in the regulation of the feeling of satiety. In addition, the drug has moderate anticholinergic properties, which contributes to its sedative effect and relaxation of smooth muscles.

The sedative effect of Periactin is due to its ability to penetrate the blood-brain barrier and affect the central nervous system, which distinguishes it from second-generation antihistamines. The effect occurs 15-30 minutes after administration and persists for 6-8 hours, depending on the dosage and individual sensitivity of the patient. The drug also demonstrates the ability to reduce migraine attacks in some patients by blocking serotonin pathways involved in migraine pathogenesis.

Pharmacokinetics

Absorption

Cyproheptadine is rapidly absorbed from the gastrointestinal tract after oral administration. The maximum concentration in blood plasma is reached in 1-3 hours, and bioavailability is about 60-70%. Food intake may slow down the rate of absorption, but does not affect the overall efficacy of the drug.

Distribution

The drug actively binds to blood plasma proteins (96-99%), mainly to albumin. The volume of distribution is about 30-40 l/kg, which indicates good penetration into tissues, including the central nervous system. This property explains the pronounced sedative effect and the ability to influence appetite through the hypothalamus.

Metabolism

Cyproheptadine is metabolized in the liver with the participation of cytochrome P450 enzymes, mainly CYP2D6 and CYP3A4. Major metabolites include hydroxylated and conjugated derivatives, which have less pharmacologic activity. The process of metabolism proceeds stepwise, providing a gradual release of the active substance and its prolonged action.

Excretion

The half-life of cyproheptadine is 6-9 hours in adults, in children it may be shorter (about 4-6 hours), and in elderly patients - longer (up to 12 hours). The drug is excreted mainly through the kidneys (about 70%) in the form of metabolites, and the remaining part - through the intestine. Less than 1% of the substance is excreted unchanged.

Indications for Use

Periactin is used for the treatment of the following conditions:

• Allergic diseases, including seasonal and year-round rhinitis, urticaria, allergic dermatitis and pruritus of various origins;
• Stimulation of appetite in anorexia, cachexia, or inadequate weight gain caused by chronic illness or recovery from illness;
• Prevention and treatment of migraine in adults and adolescents;
• Symptomatic relief of itching in eczema, insect bites or contact allergic reactions;
• Comprehensive therapy for sleep disorders associated with allergic manifestations.

The drug is particularly valuable in cases where a combination of antihistamine action and stimulation of eating behavior is required.

Contraindications

The use of Periactin is prohibited in the following conditions:

• Hypersensitivity to cyproheptadine or the excipients;
• Closed-angle glaucoma;
• Urinary retention or prostatic hyperplasia;
• Gastric or duodenal ulcer in the acute stage;
• Bronchial asthma in the acute phase;
• Pregnancy and breastfeeding period
• Children under 2 years of age.

With caution, the drug is administered to patients with epilepsy, cardiovascular diseases or severe liver and kidney dysfunction.

Method of Administration and Dosage

How to take

Periactin tablets are taken orally, drinking enough water (100-150 ml). To increase appetite, it is better to take the drug 30 minutes before a meal, and in the treatment of allergies, the time of intake is not associated with food. The syrup is measured with a measuring spoon, having previously shaken the bottle, and taken orally, also drinking water if necessary.

Dosages for adults and children

Adults

For allergies: 4 mg (1 tablet or 10 ml syrup) 3 times a day, maximum daily dose - 32 mg. For appetite stimulation: 4 mg 2 to 3 times a day.

Children from 2 to 6 years of age

Dosage is 2 mg (5 ml syrup) 2 to 3 times daily, maximum 12 mg daily.

Children 7 to 14 years of age

Recommended dosage is 4 mg (1 tablet or 10 ml syrup) 2-3 times a day, maximum - 16 mg per day.

Dose adjustment for certain conditions

In renal or hepatic insufficiency the initial dose is halved (up to 2 mg 2 times a day) with further adjustment depending on the patient's condition and under the supervision of a physician.

Side Effects

Periactin may cause the following adverse reactions:

• Nervous system: drowsiness, dizziness, weakness, confusion;
• Gastrointestinal tract: dry mouth, nausea, constipation, increased appetite;
• Cardiovascular system: tachycardia, decreased blood pressure (rare);
• Allergic reactions: rash, itching, in rare cases - Quincke's edema;
• Other: urinary retention, visual disturbances, tinnitus.

Most of the effects disappear when the dose is reduced or the body adapts to the drug.

Overdose

Symptoms of overdose

An overdose (more than 40-50 mg) may cause drowsiness, convulsions, hallucinations, respiratory depression, in severe cases - coma.

First aid measures

In case of overdose should immediately stop taking and seek help. Before the arrival of a doctor, the stomach should be washed (if it has been less than an hour) and activated charcoal should be given.

Drug Interactions

Influence on the effects of other drugs

Periactin increases the effect of sedatives, antidepressants and alcohol. Co-administration with MAO inhibitors is contraindicated due to the risk of hypertensive crisis.

Compatibility with alcohol and food

Alcohol significantly increases the sedative effect, which can be dangerous. Food does not affect efficacy, but may slow absorption.

Special Precautions

Use in pregnancy and breastfeeding

Periactin is contraindicated in pregnancy and lactation due to risk to the fetus and penetration into milk.

Effects on driving and driving mechanisms

The drug causes drowsiness, so driving and working with mechanisms are prohibited during the treatment period.

Particularities of use in the elderly and children

In the elderly, the dose is reduced due to the risk of side effects. In children use with caution, strictly observing the dosage.