Cyproheptadine 4mg Tablets

Manufacturer INGENUS PHARMACEUTICALS Active Ingredient Cyproheptadine Tablets(si proe HEP ta deen) Pronunciation si proe HEP ta deen
It is used to ease allergy signs.It is used to treat hives.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Antihistamine, Appetite Stimulant
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Pharmacologic Class
First-generation H1-receptor antagonist, Serotonin antagonist
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Pregnancy Category
Category B
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FDA Approved
Mar 1961
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Cyproheptadine is an antihistamine that helps relieve allergy symptoms like sneezing, runny nose, and itchy eyes. It can also increase appetite in some people. It works by blocking certain natural substances (histamine and serotonin) in your body.
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How to Use This Medicine

Taking Your Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food. If it causes stomach upset, taking it with food may help.

Storing and Disposing of Your Medication

Keep your medication at room temperature in a dry place, away from the bathroom. Store all medications in a safe location, out of reach of children and pets.

Missing a Dose

If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Do not take two doses at the same time or take extra doses.
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Lifestyle & Tips

  • Avoid driving or operating heavy machinery until you know how this medication affects you, as it can cause drowsiness or dizziness.
  • Avoid alcohol and other CNS depressants (e.g., sedatives, tranquilizers) while taking this medication, as they can increase drowsiness.
  • To relieve dry mouth, suck on sugarless candy or ice chips, or use a saliva substitute.
  • If taking for appetite stimulation, maintain a balanced diet and consult with a healthcare provider or dietitian.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: 4 mg three to four times daily
Dose Range: 4 - 20 mg

Condition-Specific Dosing:

Allergies: 4 mg three times daily, up to 20 mg/day
Appetite Stimulation: 4 mg three to four times daily, up to 20 mg/day
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Pediatric Dosing

Neonatal: Not established
Infant: Not established (contraindicated in newborns/premature infants)
Child: 2-6 years: 2 mg two to three times daily (max 12 mg/day); 7-14 years: 4 mg two to three times daily (max 16 mg/day)
Adolescent: Same as adult dosing for allergies/appetite stimulation, typically 4 mg three times daily
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment, use with caution
Moderate: Use with caution, consider lower doses
Severe: Use with caution, consider lower doses due to potential accumulation of metabolites
Dialysis: Not well studied, use with caution; likely not dialyzable due to high protein binding

Hepatic Impairment:

Mild: Use with caution
Moderate: Use with caution, consider lower doses due to extensive hepatic metabolism
Severe: Contraindicated in severe hepatic impairment
Confidence: Medium

Pharmacology

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Mechanism of Action

Cyproheptadine is a first-generation antihistamine that competitively antagonizes H1-receptors, thereby blocking the effects of histamine. It also possesses significant antiserotonergic (5-HT2 receptor antagonism) and anticholinergic properties. Its appetite-stimulating effect is thought to be related to its antiserotonergic activity on the hypothalamus.
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Pharmacokinetics

Absorption:

Bioavailability: Well absorbed orally, but specific percentage not widely reported
Tmax: 1-3 hours
FoodEffect: Food may slightly delay absorption but does not significantly affect bioavailability.

Distribution:

Vd: Not widely reported, but widely distributed throughout the body
ProteinBinding: Approximately 96%
CnssPenetration: Yes

Elimination:

HalfLife: 8-16 hours (variable)
Clearance: Not widely reported
ExcretionRoute: Mainly urine (2-20% unchanged drug, remainder as metabolites), some via feces
Unchanged: 2-20%
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Pharmacodynamics

OnsetOfAction: 15-60 minutes
PeakEffect: 1-3 hours
DurationOfAction: 4-8 hours
Confidence: Medium

Safety & Warnings

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Side Effects

Serious Side Effects: Seek Medical Attention Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical help right away:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Severe dizziness or fainting
Abnormal or rapid heartbeat
Difficulty urinating
Changes in urination frequency
Confusion
Balance problems
Hallucinations (seeing or hearing things that are not there)
Irritability
Mood changes
Seizures
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling extremely tired or weak
Abnormal sensations, such as burning, numbness, or tingling
Changes in vision
Ringing in the ears
Excessive sweating
Changes in menstrual cycle

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:

Dizziness, drowsiness, tiredness, or weakness
Headache
Constipation, diarrhea, stomach pain, upset stomach, vomiting, or decreased appetite
Increased appetite
Weight gain
Dry mouth
Dry nose
Stuffy nose
Feeling nervous or excitable
Restlessness
Shakiness
Sleep disturbances

Reporting Side Effects

This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Severe drowsiness or dizziness
  • Confusion or hallucinations
  • Difficulty urinating
  • Severe dry mouth or blurred vision
  • Rapid or irregular heartbeat
  • Seizures
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following conditions and circumstances before starting this medication:

If you have a known allergy to cyproheptadine or any other component of this medication. Describe your allergic reaction and the symptoms you experienced.
If you have any of the following health conditions:
+ Bowel obstruction
+ Enlarged prostate
+ Glaucoma
+ Difficulty urinating
+ Stomach or bowel ulcers
If you are taking certain medications, such as:
+ Isocarboxazid, phenelzine, or tranylcypromine (used to treat depression)
+ Selegiline or rasagiline (used to treat Parkinson's disease)
+ Linezolid or methylene blue
If you are 65 years or older
If you are breastfeeding. Note: You should not breastfeed while taking this medication.

Special Considerations for Children:

If your child is a premature baby or a newborn, do not administer this medication. It is not suitable for premature babies or newborns.

Additional Important Information:

This list is not exhaustive, and it is crucial to inform your doctor and pharmacist about all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions. This will help ensure your safety while taking this medication. Never start, stop, or change the dose of any medication without consulting your doctor first.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

Until you are aware of how this drug affects you, avoid operating a vehicle or engaging in any activities that require alertness.

This medication may interfere with the results of allergy skin tests. Therefore, it is crucial to notify your doctor and laboratory personnel that you are taking this drug.

Before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may cause drowsiness, consult with your doctor.

Be cautious when exposed to sunlight, as this medication may increase your susceptibility to sunburn. If you experience excessive sunburn while taking this medication, notify your doctor.

It is critical to exercise caution when administering this medication to children, as overdoses can occur and may lead to severe health complications or even death. If you have any questions or concerns, discuss them with your doctor.

Additionally, children should use this medication with caution, and it is recommended that you consult with your doctor.

If you are pregnant or planning to become pregnant, inform your doctor, as it is necessary to discuss the potential benefits and risks associated with using this medication during pregnancy.
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Overdose Information

Overdose Symptoms:

  • Severe drowsiness or deep sleep
  • Coma
  • Ataxia (loss of coordination)
  • Dizziness
  • Weakness
  • Blurred vision
  • Dilated pupils
  • Dry mouth
  • Flushed skin
  • Fever
  • Agitation
  • Hallucinations
  • Seizures
  • Tachycardia (rapid heart rate)
  • Hypotension (low blood pressure)
  • Urinary retention
  • Bowel obstruction

What to Do:

Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is supportive and symptomatic, including gastric lavage, activated charcoal, and management of anticholinergic symptoms (e.g., physostigmine in severe cases under medical supervision).

Drug Interactions

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Contraindicated Interactions

  • Monoamine Oxidase Inhibitors (MAOIs) - concurrent use or within 14 days of MAOI discontinuation (potentiates anticholinergic effects)
  • Severe hepatic impairment
  • Newborns or premature infants
  • Nursing mothers
  • Elderly, debilitated patients with glaucoma, prostatic hypertrophy, bladder neck obstruction, pyloroduodenal obstruction
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Major Interactions

  • CNS Depressants (e.g., alcohol, sedatives, hypnotics, anxiolytics, opioids, tricyclic antidepressants, other antihistamines) - additive CNS depression
  • Anticholinergic drugs (e.g., atropine, tricyclic antidepressants, phenothiazines) - additive anticholinergic effects (dry mouth, blurred vision, urinary retention, constipation)
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Moderate Interactions

  • Topical antihistamines - additive systemic effects
  • Potassium chloride (oral) - increased risk of GI lesions due to anticholinergic effects
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Minor Interactions

  • None specifically noted as minor, but general caution with any drug affecting CNS or anticholinergic activity.

Monitoring

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Baseline Monitoring

Baseline symptoms (e.g., allergy symptoms, weight if used for appetite)

Rationale: To assess efficacy and track progress

Timing: Prior to initiation

Mental status/level of consciousness

Rationale: To assess baseline CNS function due to potential for sedation

Timing: Prior to initiation

Renal and hepatic function (if comorbidities exist)

Rationale: To identify patients at higher risk for accumulation or adverse effects

Timing: Prior to initiation, especially in elderly or those with known impairment

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Routine Monitoring

Efficacy (e.g., symptom relief for allergies, weight gain for appetite stimulation)

Frequency: Periodically, as clinically indicated

Target: Symptom resolution, desired weight gain

Action Threshold: Lack of efficacy or excessive side effects

Adverse effects (e.g., sedation, dry mouth, blurred vision, urinary retention, constipation)

Frequency: Regularly, especially during initial therapy and dose adjustments

Target: Minimal to tolerable side effects

Action Threshold: Intolerable side effects, severe CNS depression, or signs of anticholinergic toxicity

Weight (if used for appetite stimulation)

Frequency: Weekly to monthly

Target: Gradual, healthy weight gain

Action Threshold: No weight gain or excessive, rapid weight gain

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Symptom Monitoring

  • Drowsiness
  • Dizziness
  • Dry mouth
  • Blurred vision
  • Urinary retention
  • Constipation
  • Nervousness
  • Irritability
  • Confusion (especially in elderly)
  • Paradoxical excitation (especially in children)

Special Patient Groups

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Pregnancy

Category B. Animal reproduction studies have shown no risk to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed.

Trimester-Specific Risks:

First Trimester: Generally considered low risk, but caution advised.
Second Trimester: Generally considered low risk.
Third Trimester: Generally considered low risk, but potential for CNS effects in neonate if used close to delivery.
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Lactation

Not recommended. Cyproheptadine is excreted in breast milk and may cause sedation or other adverse effects in the nursing infant. It may also inhibit lactation due to its anticholinergic effects.

Infant Risk: Moderate to high risk (sedation, irritability, anticholinergic effects, potential for decreased milk supply).
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Pediatric Use

Contraindicated in newborns and premature infants. Use with caution in children due to potential for paradoxical excitation (restlessness, irritability) or increased sensitivity to anticholinergic effects. Dosage must be carefully calculated based on age and weight.

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Geriatric Use

Use with extreme caution. Elderly patients are more susceptible to the anticholinergic effects (e.g., dry mouth, urinary retention, constipation, blurred vision) and CNS effects (e.g., sedation, dizziness, confusion, hypotension) of cyproheptadine. Lower doses are often recommended, and it is generally considered a potentially inappropriate medication in the elderly according to Beers Criteria.

Clinical Information

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Clinical Pearls

  • Cyproheptadine is a first-generation antihistamine with significant anticholinergic and antiserotonergic properties, leading to its use for both allergies and appetite stimulation.
  • Sedation is a common and often dose-limiting side effect; advise patients to avoid activities requiring mental alertness.
  • Paradoxical excitation can occur, especially in children, manifesting as restlessness, insomnia, or nervousness.
  • Due to its anticholinergic effects, it should be used with caution or avoided in patients with glaucoma, prostatic hypertrophy, or urinary retention.
  • Its use as an appetite stimulant is off-label in many regions but is a common clinical practice, particularly in pediatric populations or those with chronic illness-related cachexia.
  • Tolerance to the sedative effect may develop over time, but anticholinergic effects may persist.
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Alternative Therapies

  • Other first-generation antihistamines (e.g., diphenhydramine, chlorpheniramine) for allergy symptoms (though less potent antiserotonergic effects)
  • Second-generation antihistamines (e.g., loratadine, cetirizine, fexofenadine) for allergy symptoms (less sedating, minimal anticholinergic effects)
  • Mirtazapine (antidepressant with appetite-stimulating properties)
  • Dronabinol (cannabinoid, appetite stimulant for specific conditions)
  • Megestrol acetate (progestin, appetite stimulant for specific conditions)
  • Nutritional counseling and dietary interventions for appetite/weight gain
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Cost & Coverage

Average Cost: $10 - $30 per 30 tablets
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (Generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, including the amount and time of ingestion.