'Periactin' is a serotonin and histamine antagonist with anticholinergic and sedative properties.

 

 

In allergy and pruritus: 'Periactin' has a wide range of anti-allergic and antipruritic activity, and can be used successfully in the treatment of acute and chronic allergic and pruritic conditions, such as dermatitis, including neurodermatitis and neurodermatitis circumscripta; eczema; eczematoid dermatitis; dermatographism; mild, local allergic reactions to insect bites; hay fever and other seasonal rhinitis; perennial allergic and vasomotor rhinitis; allergic conjunctivitis due to inhalant allergens and foods; urticaria; angioneurotic oedema; drug and serum reactions; anogenital pruritus; pruritus of chicken-pox.

 

'Periactin' is indicated as adjunctive therapy to adrenaline and other standard measures for the relief of anaphylactic reactions after the acute manifestations have been controlled.

 

In migraine and vascular headache: 'Periactin' has been reported to have beneficial effects in a significant number of patients having vascular types of headache. Many patients who have responded  inadequately  to  all  other  agents  have  reported  amelioration  of  symptoms  with 'Periactin'. The characteristic headache and feeling of malaise may disappear within an hour or two of the first dose.

 

Route of administration: oral.

 

 

There is no recommended dosage for children under 2 years old. 'Periactin' is not recommended for elderly, debilitated patients.

 

For the treatment of allergy and pruritus:

 

 

Dosage must be determined on an individual basis. The effect of a single dose usually lasts for four to six hours. For continuous effective relief, the daily requirement should be given in divided doses, usually three times a day, or as often as necessary, to provide continuous relief.

 

Adults: The therapeutic range is 4-20 mg (1 to 5 tablets) a day, most patients requiring 12-16 mg a day. It is recommended that dosage be initiated with 4 mg three times a day and then adjusted according to the weight and response of the patient up to a maximum of 32 mg a day.

 

Children aged 7-14 years: Usually 4 mg two or three times a day, according to the patient's weight and response. If an additional dose is required, it should be given at bedtime. Maximum

16 mg a day.

 

 

Children aged 2-6 years: Initially 2 mg two or three times a day, adjusted according to the patient's weight and response. If an additional dose is required, it should be given at bedtime.

Maximum 12 mg a day.

 

For treatment of vascular headache and migraine:

 

 

For both prophylactic and therapeutic use, an initial dose of 4 mg, repeated if necessary after half an hour. Patients who respond usually obtain relief with 8 mg, and this dose should not be  exceeded within a 4- to 6-hour period.

 

Maintenance: 4 mg every four to six hours.

Use in the elderly: 'Periactin' should not be used in elderly, debilitated patients. Elderly patients are more likely to experience dizziness, sedation, and hypotension.

 

'Periactin' is contraindicated in: • patients undergoing therapy for an acute asthmatic attack; • newborn or premature infants; use in infants has been associated with apnoea, cyanosis and respiratory difficulty • breast-feeding mothers; • patients with known sensitivity to cyproheptadine hydrochloride or drugs with similar chemical structure; • concurrent use with monoamine oxidase inhibitors; • glaucoma; • patients with pyloroduodenal obstruction, stenosing peptic ulcer, symptomatic prostatic hypertrophy, predisposition to urinary retention or bladder neck obstruction; • elderly, debilitated patients.

Antihistamines should not be used to treat lower respiratory tract symptoms, including those of acute asthma.

 

The safety and efficacy of 'Periactin' is not established in children under 2 years old.

 

 

Overdosage of antihistamines, particularly in infants and children, may produce hallucinations, central nervous system depression, convulsions, respiratory and cardiac arrest, and death.

 

Antihistamines may diminish mental alertness; conversely, particularly in the young child, they may occasionally produce excitation.

Patients  should  be warned  against  engaging  in  activities  requiring motor co-ordination  and mental alertness, such as driving a car or operating machinery (see section 4.7 'Effects on ability to drive and use machines').

 

Rarely, prolonged therapy with antihistamines may cause blood dyscrasias.

 

 

Because 'Periactin' has an atropine-like action, it should be used cautiously in patients with a history of bronchial asthma, increased intra-ocular pressure, hyperthyroidism, cardiovascular disease, or hypertension.

MAO inhibitors prolong and intensify the anticholinergic effects of antihistamines.

 

 

Antihistamines  may  have  additive  effects  with  alcohol  and  other  CNS  depressants,  e.g.

hypnotics, sedatives, tranquillisers and anti-anxiety agents.

 

Drugs with anti-serotonin activity, such as cyproheptadine, may interfere with serotonin- enhancing anti-depressants including selective serotonin re-uptake inhibitors (SSRI's). This may result in possible recurrence of depression and related symptoms.

 

Cyproheptadine may cause a false positive test result for tricyclic antidepressant drugs (TCA) when evaluating a drug screen (e.g. urine, serum). Because cyproheptadine and TCAs may produce similar overdose symptoms, physicians should carefully monitor patients for TCA toxicity in the event of combined overdose.

The use of any drug in pregnancy or in women of child-bearing age requires that the potential benefit of the drug should be weighed against possible hazards to the embryo and foetus. It is not known whether 'Periactin' is excreted in human milk, and because of the potential for serious adverse reactions in breast-feeding infants from 'Periactin', a decision should be made whether to discontinue breast-feeding or to discontinue the drug, taking into account the importance of the drug to the mother (see section 4.3 'Contraindications').

 

This product may cause drowsiness and somnolence. Patients receiving it should not drive or operate machinery unless it has been shown that their physical and mental capacity remains unaffected.

The side effects that appear frequently are drowsiness and somnolence. Many patients who initially complain of drowsiness may no longer do so after the first three to four days of continuous administration.

 

Side effects reported with antihistamines are:

 

 

Central nervous system: Sedation, sleepiness (often transient), dizziness, disturbed co-ordination, confusion, restlessness, excitation, nervousness, tremor, irritability, aggressive behaviour, insomnia, paraesthesiae, neuritis, convulsions, euphoria, hallucinations, hysteria, faintness.

 

Integumentary: Allergic manifestations of rash and oedema, excessive perspiration, urticaria, photosensitivity.

 

Special senses: Acute labyrinthitis, blurred vision, diplopia, vertigo, tinnitus.

Cardiovascular: Hypotension, palpitation, tachycardia, extrasystoles, anaphylactic shock.

Haematological: Haemolytic anaemia, leucopenia, agranulocytosis, thrombocytopenia.

Digestive system: Cholestasis, hepatic failure, hepatitis, hepatic function abnormality, dryness of mouth, epigastric distress, anorexia, nausea, vomiting, diarrhoea, constipation, jaundice.

 

Genito-urinary: Frequency and difficulty of micturition, urinary retention, early menses.

 

 

Respiratory: Dryness of the nose and throat, thickening of bronchial secretions, tightness of chest and wheezing, nasal stuffiness, epistaxis.

 

Miscellaneous: Fatigue, rigors, headache, increased appetite/weight gain.

To report any side effect(s):

Saudi Arabia: National Pharmacovigilance and Drug Safety Center (NPC)

•   Call NPC at +966-11-2038222, Exts: 2317-2356-2353-2354-2334-2340

•   Fax: +966-11-205-7662

•   Toll-free: 8002490000

•   Email: npc.drug@sfda.gov.sa

Website: www. sfda.gov.sa/npc

Antihistamine  overdosage  reactions  may  vary  from  CNS  depression  or  stimulation  to convulsions,  respiratory  and  cardiac  arrest  and  death,  especially  in  infants  and  children.

Atropine-like and gastro-intestinal symptoms may occur.

 

If vomiting has not occurred spontaneously, it should be induced in the conscious patient with syrup of ipecac. If the patient cannot vomit, gastric lavage with isotonic or half isotonic saline is indicated,  followed  by  activated  charcoal.  Precautions  against  aspiration  must  be  taken, especially in infants and children.

 

Life-threatening CNS signs and symptoms should be treated appropriately.

 

 

Saline cathartics usefully draw water into the bowel by osmosis to dilute bowel content rapidly.

Central stimulants must not be used, but vasopressors may be used to counteract hypotension.

 

 

Cyproheptadine hydrochloride is a serotonin and histamine antagonist with anticholinergic and sedative effects. Antiserotonin and antihistamine drugs appear to compete with serotonin and histamine, respectively, for receptor sites.

 

Cyproheptadine  hydrochloride  antagonises  the  following  effects  of  serotonin,  in  laboratory animals:

 

Bronchoconstrictor (guinea-pig)

Vasopressor (dog)

Spasmogenic (isolated rat uterus)

Oedema (rat)

Lethal (haemophilus pertussis-treated mouse)

 

In these effects it equals or surpasses the activity of many of the activities of specific serotonin antagonists, such as 1-Benzyl-2-methyl-5-methoxy-tryptame (BAS) and 1 Benzyl-2methyl-5- hydroxy-tryptamine (BMS), in contrast, specific antihistamines, even the most potent, show little or no serotonin antagonism.

 

Cyproheptadine hydrochloride antagonises or blocks the following effects of histamine in laboratory animals:

 

Bronchoconstrictor (guinea-pig)

Vasopressor (dog)

Spasmogenic (isolated rat uterus)

 

 

Anaphylactic shock, active and passive (guinea-pig and mouse)

Increased gastric secretion (Heidenhain pouch dog.)

It is unusual that cyproheptadine hydrochloride protects both the guinea-pig and mice against anaphylactic shock. In guinea-pigs, the pulmonary aspects of anaphylactic shock are attributable to the release of endogenous histamine and can be controlled by substances with specific antihistamine activity. In mice however, where histamine release seems to be less important and serotonin release may be involved, specific antihistamines are of little value in protecting against anaphylaxis. Thus the protective effect of cyproheptadine hydrochloride in mice may be an anti- serotonin effect.

 

The inhibitory effect of cyproheptadine in histamine-induced gastric secretion is also unusual as specific antihistamines do not influence this effect.

 

Cyproheptadine has appetite stimulation properties in laboratory animals.

 

 

After a single 4 mg oral dose of ¹⁴C-labelled cyproheptadine hydrochloride in normal subjects given as tablets or syrup, 2 to 20% of the radioactivity was excreted in the stools. Only about

34% of the stool radioactivity was unchanged drug, corresponding to less than 5.7% of the dose.

At least 40% of the administered radioactivity was excreted in the urine.

No significant difference in the mean urinary excretion exists between the tablet and syrup formulations. No detectable amounts of unchanged drug were present in the urine of patients on chronic 12-20 mg daily doses of 'Periactin' syrup. The principle metabolite found in human urine has been identified as a quaternary ammonium glucuronide conjugate of cyproheptadine.

Elimination is diminished in renal insufficiency.

No relevant information.

 

Dibasic  calcium  phosphate  hydrous,  lactose  hydrous,  potato  starch,  pregelatinated  starch, magnesium stearate.

None known.

3 years.

Do not store above 30°C.

 

PVC/Al blisters, 10 strips of 10 tablets

None.