Heptadine

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

Heptadine 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.

Heptadine 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 Heptadine
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 Franklin Laboratories (india) Pvt Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Heptadine
Heptadine

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.

Heptadine 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 Heptadine works

Heptadine 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

Heptadine 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 Heptadine

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

FAQ

What is Heptadine used for?

Heptadine is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. Heptadine 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 Heptadine?

Do not use Heptadine 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 Heptadine work?

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

What are the common side effects of Heptadine?

Common sid effects of Heptadine are include:

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

Is Heptadine safe during pregnancy?

Heptadine 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 Heptadine safe during breastfeeding?

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

Can I drink alcohol with Heptadine?

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

When is the best time to take Heptadine?

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

How many times a day can I take Heptadine?

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

How long does Heptadine to start working?

Heptadine 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 Heptadine?

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 Heptadine?

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 Heptadine stay in my system?

Heptadine 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 Heptadine?

You should stop taking Heptadine once your symptoms have eased.

What should if I miss a dose of Heptadine?

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 Heptadine affect liver?

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

How long does Heptadine last?

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

Does Heptadine cause weight gain?

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

Does Heptadine affect my period?

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

Can Heptadine increase blood pressure?

Heptadine therapy significantly improved systolic and diastolic blood pressure.

Does Heptadine affect the kidneys?

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

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0002448
http://classyfire.wishartlab.com/tax_nodes/C0000019
http://classyfire.wishartlab.com/tax_nodes/C0000019
http://classyfire.wishartlab.com/tax_nodes/C0000195
http://classyfire.wishartlab.com/tax_nodes/C0002239
http://classyfire.wishartlab.com/tax_nodes/C0004139
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:4046
http://www.hmdb.ca/metabolites/HMDB0014578
http://www.genome.jp/dbget-bin/www_bget?cpd:C06935
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2913
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508613
https://www.chemspider.com/Chemical-Structure.2810.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50017721
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=3013
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=4046
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL516
https://zinc.docking.org/substances/ZINC000000968264
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000103
http://www.pharmgkb.org/drug/PA164749366
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=277
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/C7H
http://www.rxlist.com/cgi/generic2/cyprohept.htm
https://www.drugs.com/cdi/cyproheptadine.html
https://en.wikipedia.org/wiki/Cyproheptadine
*** Taking medicines without doctor's advice can cause long-term problems.
Share