Apetol

Apetol Uses, Dosage, Side Effects, Food Interaction and all others data.

Apetol is a sedating antihistamine with antimuscarinic, serotonin antagonist and Ca channel blocking properties. It competes with histamine for H1-receptor sites on effector cells in the GI tract, blood vessels and resp tract.

Apetol has been observed to antagonize several pharmacodynamic effects of serotonin in laboratory animals, including bronchoconstriction and vasodepression, and has demonstrated similar efficacy in antagonizing histamine-mediated effects. The reason for its efficacy in preventing anaphylactic shock has not been elucidated, but appears to be related to its anti-serotonergic effects.

Trade Name Apetol
Availability Prescription only
Generic Cyproheptadine
Cyproheptadine Other Names Ciproheptadina, Cyproheptadin, Cyproheptadine, Cyproheptadinum
Related Drugs Ubrelvy, Botox, prednisone, hydroxyzine, diclofenac, cetirizine, loratadine, fluticasone nasal, dexamethasone, promethazine
Type Syrup
Formula C21H21N
Weight Average: 287.3981
Monoisotopic: 287.167399677
Groups Approved
Therapeutic Class Sedating Anti-histamine
Manufacturer Menper Distributors
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Apetol
Apetol

Uses

  • Perenial and seasonal allergic rhinitis
  • Vasomotor rhinitis
  • Allergic conjunctivitis due to inhalant allergens and foods
  • Mild, uncomplicated allergic skin manifestations of urticaria and angioedema
  • Amelioration of allergic reactions to blood or plasma
  • Cold urticaria
  • Dermatographism

As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled.

Apetol is also used to associated treatment for these conditions: Allergic Reactions caused by Transfusions, Anaphylaxis, Angioedema and urticaria, Cold urticaria, Conjunctivitis allergic caused by Food Allergy, Conjunctivitis allergic caused by inhalant allergens, Perennial Allergic Rhinitis (PAR), Pruritus, Seasonal Allergic Rhinitis, Serotonin Syndrome, Vasomotor Rhinitis, Dermatographism, Appetite stimulation

How Apetol works

Apetol appears to exert its antihistamine and antiserotonin effects by competing with free histamine and serotonin for binding at their respective receptors. Antagonism of serotonin on the appetite center of the hypothalamus may account for cyproheptadine's ability to stimulate the appetite.

Dosage

Apetol dosage

Pediatric Patients:Age 2 To 6 Years:

  • The total daily dosage for pediatric patients may be calculated on the basis of body weight or body area using approximately 0.25 mg/kg/day or 8 mg per square meter of body surface (8 mg/m2).
  • The usual dose is 2 mg two or three times a day, adjusted as necessary to the size and response of the patient. The doe is not to exceed 12 mg a day.

Age 7 To 14 Years:

  • The usual dose is 4 mg two or three times a day adjusted as necessary to the size and response of the patient. The dose is not to exceed 16 mg a day.

Adults: The total daily dose for adults should bot exceed 0.5 mg/kg/day. The therapeutic range is 4 to 20 mg a day, with the majority of patients requiring 12 to 16 mg a day. An occasional patient may require as much as 32 mg a day for adequate relief. It is suggested that dosage be initiated with 4 mg three times a day and adjusted according to the size and response of the patient.

Side Effects

Confusion, disturbed coordination, dizziness, excitation, euphoria, hallucinations, headache, hysteria, insomnia, irritability, nervousness, restlessness, sedation, seizure, sleepiness, tremor, vertigo, hypotension, palpitation, tachycardia, abdominal pain, anorexia, increased appetite, constipation, diarrhoea, nausea, vomiting, xerostomia, difficult urination, urinary retention, urinary frequency, blurred vision, diplopia, tinnitus, acute labyrinthitis, nasal congestion, pharyngitis, thickening bronchial secretion, paraesthesia, hepatitis, cholestasis, hepatic failure, jaundice, angioedema, photosensitivity, rash, urticaria, fatigue, chills, diaphoresis.

Toxicity

Overdosage with cyproheptadine is likely to result in significant sedation - although paradoxical stimulation has been noted in pediatric patients - and anticholinergic adverse effects such as dry mouth and flushing. Most patients appear to recover without incident, as a review of cyproheptadine overdose cases in Hong Kong found the majority of patients had no or mild symptoms following intentional overdose.

In the event of overdosage with cyproheptadine, prescribing information recommends the induction of vomiting (if it has not occurred spontaneously) using syrup of ipecac. Gastric lavage and activated charcoal may also be considered. Vasopressors may be used to treat hypotension and intravenous physostigmine salicylate may be considered for the treatment of significant CNS symptoms depending on the clinical picture.

Precaution

Patient with CV disease including HTN and ischaemic heart disease, increased intraocular pressure, asthma or other chronic breathing disorders, thyroid dysfunction. Pregnancy.

Interaction

May have additive effects with CNS depressants e.g. hypnotics, sedatives, tranquilizers, antianxiety agents. MAOIs prolong and intensify the anticholinergic effects of antihistamines.

Food Interaction

  • Avoid alcohol. Co-administration with alcohol may potentiate the sedative effects of cyproheptadine.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Elimination Route

A single study examining the difference in absorption of orally administered versus sublingually administered cyproheptadine in five healthy males demonstrated a mean Cmax of 30.0 mcg/L and 4.0 mcg/L, respectively, and a mean AUC of 209 mcg.h/L and 25 mcg.h/L, respectively. The Tmax of orally and sublingually administered cyproheptadine was 4 hours and 9.6 hours, respectively.

Elimination Route

Approximately 2-20% of the radioactivity from an orally administered radio-labeled dose of cyproheptadine is excreted in the feces, of which approximately 34% is unchanged parent drug (less than 5.7% of the total dose). At least 40% of radioactivity is recovered in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category B. Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Contraindication

Narrow-angle glaucoma, bladder neck obstruction, pyloroduodenal obstruction, symptomatic prostatic hyperplasia, stenosing peptic ulcer. Concurrent use with MAOIs. Debilitated elderly, newborn or premature infants. Lactation.

Acute Overdose

Symptoms: CNS depression to stimulation, atropine-like (e.g. dry mouth, fixed, dilated pupils, flushing) and GI symptoms.

Management: Induce vomiting with syrup of ipecac. If unable to vomit, perform gastric lavage followed by activated charcoal. Saline cathartics may be useful for quick dilution of bowel content by osmosis. Vasopressors may be used for hypotension.

Storage Condition

Store between 15-30°C.

Innovators Monograph

You find simplified version here Apetol

Apetol contains Cyproheptadine see full prescribing information from innovator Apetol Monograph, Apetol MSDS, Apetol FDA label

FAQ

What is Apetol used for?

Apetol is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. Apetol is used to relieve allergy symptoms such as watery eyes, runny nose, itching eyes/nose, sneezing, hives, and itching. It may also be used to relieve the itching of allergic skin conditions, including hives caused by exposure to cold temperatures and by rubbing the skin.

How safe is Apetol?

Do not use Apetol in larger or smaller amounts or for longer than recommended. Do not give this medicine to a child younger than 2 years old. You should not use antihistamine medication to make a child sleepy. Death can occur from the misuse of an antihistamine in very young children.

How does Apetol work?

Apetol works by blocking the action of histamine, a substance in the body that causes allergic symptoms.

What are the common side effects of Apetol?

Common sid effects of Apetol are include:

dry mouth, nose, and throat.
drowsiness.
dizziness.
nausea.
chest congestion.
headache.
excitement (especially in children)
muscle weakness.

Is Apetol safe during pregnancy?

Apetol is not expected to be harmful to an unborn baby. Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women. Use is recommended only if clearly needed and the benefit outweighs the risk.

Is Apetol safe during breastfeeding?

Apetol is contraindicated in breastfeeding due to its potential effects on lactation.

Can I drink alcohol with Apetol?

You should avoid or limit the use of alcohol while being treated with Apetol.

When is the best time to take Apetol?

Apetol is usually taken two or three times a day. You can take Apetol before or after meals. Take Apetol at around the same time(s) every day.

How many times a day can I take Apetol?

You can take Apetol usually 2 to 3 times a day.

How long does Apetol to start working?

Apetol should help your animal feel better within 1 to 2 hours. Your animal's clinical signs should improve after that time.

What happens when I take Apetol?

Drowsiness, dizziness, blurred vision, constipation, or dry mouth/nose/throat may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

What happen if I overdose on Apetol?

Overdose symptoms may include extreme drowsiness, hallucinations, very dry mouth, dilated pupils, pale or reddish skin, tingly feeling, vomiting, restlessness (in a child), weak or shallow breathing, or a seizure (convulsions).

How long does Apetol stay in my system?

Apetol is well-absorbed following oral ingestion, with peak plasma levels occurring after 1 to 3 hours. Its terminal half-life when taken orally is approximately 8 hours.

Can I just stop taking Apetol?

You should stop taking Apetol once your symptoms have eased.

What should if I miss a dose of Apetol?

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Does Apetol affect liver?

Apetol has been associated with several instances of clinically apparent liver injury.

How long does Apetol last?

Apetol usually acts within 2 hours. Don't take too much, as the sleepiness and grogginess can last 12 to 18 hours.

Does Apetol cause weight gain?

Apetol may benefit those at risk of malnutrition, it could lead to excessive weight gain in overweight people or those with a healthy weight.

Does Apetol affect my period?

Ten of the 15 women had menstrual bleeding while receiving Apetol, seven had decreased galactorrhea, and two had cessation of galactorrhea. The side effects of treatment were transient drowsiness and weight gain.

Can Apetol increase blood pressure?

Apetol therapy significantly improved systolic and diastolic blood pressure.

Does Apetol affect the kidneys?

Despite prolonged survival, Apetol-treated animals usually showed the histological findings of acute and chronic renal rejection.

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*** Taking medicines without doctor's advice can cause long-term problems.
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