Cyproheptadine 2mg/5ml Syrup

Manufacturer QUAGEN PHARMACEUTICALS Active Ingredient Cyproheptadine Syrup(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, Antiserotonergic
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Pharmacologic Class
H1-receptor antagonist, Anticholinergic, Antiserotonergic
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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 make some people feel hungry, so it's sometimes used to help with appetite. It often causes drowsiness.
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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. When measuring liquid doses, use the measuring device that comes with the medication. If one is not provided, ask your pharmacist for a suitable measuring device.

Storing and Disposing of Your Medication

Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets, to prevent accidental ingestion.

What to Do If You Miss 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 resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
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Lifestyle & Tips

  • Avoid alcohol and other medications that cause drowsiness, as this can worsen sedation.
  • Be cautious when driving or operating machinery until you know how this medication affects you.
  • To relieve dry mouth, suck on sugarless candy or ice chips, or use artificial saliva.
  • Take with food or milk if stomach upset occurs.
  • Avoid prolonged exposure to sunlight or tanning beds, as this medication may increase sensitivity to the sun.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: 4 mg orally 3 times a day for allergic conditions
Dose Range: 4 - 20 mg

Condition-Specific Dosing:

allergic_conditions: 4 mg orally 3 times a day; range 4-20 mg/day in divided doses, not to exceed 0.5 mg/kg/day.
appetite_stimulation_off_label: 2-4 mg orally 3-4 times a day.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established (contraindicated in neonates/premature infants)
Child: 2-6 years: 2 mg orally 2-3 times a day (max 12 mg/day). 7-14 years: 4 mg orally 2-3 times a day (max 16 mg/day). For appetite stimulation (off-label): 0.25 mg/kg/day divided into 2-3 doses.
Adolescent: Same as adult dosing for allergic conditions (4 mg orally 3 times a day; range 4-20 mg/day in divided doses).
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Dose Adjustments

Renal Impairment:

Mild: Use with caution; dose adjustment may be necessary due to renal excretion of metabolites.
Moderate: Use with caution; dose adjustment likely necessary. Start with lower end of dosing range.
Severe: Use with caution; dose adjustment likely necessary. Consider significant dose reduction.
Dialysis: Not well studied; use with caution. Metabolites are renally excreted.

Hepatic Impairment:

Mild: Use with caution; dose adjustment may be necessary due to hepatic metabolism.
Moderate: Use with caution; dose adjustment likely necessary. Start with lower end of dosing range.
Severe: Use with caution; significant dose reduction likely necessary. Avoid if possible.
Confidence: Medium

Pharmacology

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Mechanism of Action

Cyproheptadine is a first-generation antihistamine that competitively blocks H1-histamine receptors. It also possesses significant antiserotonergic activity (blocking 5-HT2 receptors) and anticholinergic properties. Its appetite-stimulating effect is thought to be related to its antiserotonergic activity.
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Pharmacokinetics

Absorption:

Bioavailability: Not precisely quantified, but well absorbed orally.
Tmax: Approximately 6-9 hours
FoodEffect: Food does not significantly affect absorption, but may reduce GI upset.

Distribution:

Vd: Not precisely quantified, but widely distributed.
ProteinBinding: Approximately 96%
CnssPenetration: Yes (readily crosses the blood-brain barrier, contributing to sedation)

Elimination:

HalfLife: Approximately 8 hours
Clearance: Not precisely quantified
ExcretionRoute: Primarily renal (as metabolites), with some fecal excretion.
Unchanged: < 2% (renal)
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Pharmacodynamics

OnsetOfAction: 15-60 minutes
PeakEffect: 6-9 hours
DurationOfAction: Approximately 8 hours

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

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 attention immediately:

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
Menstrual changes

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
Nervousness and excitability
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, contact 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
  • Difficulty urinating
  • Severe constipation
  • Blurred vision or eye pain
  • Confusion or hallucinations
  • Unusual excitement or nervousness (especially in children)
  • Yellowing of skin or eyes (jaundice)
  • Unusual bleeding or bruising
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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 situations to ensure safe treatment with this medication:

Allergies: If you have a known allergy to cyproheptadine or any other component of this medication, inform your doctor. Describe the allergic reaction and any symptoms you experienced.
Health conditions: Tell your doctor if you have any of the following health problems:
+ Bowel blockage
+ Enlarged prostate
+ Glaucoma
+ Difficulty passing urine
+ Stomach or bowel ulcers
Medications: Inform your doctor if you are taking:
+ Certain antidepressant medications, such as isocarboxazid, phenelzine, or tranylcypromine
+ Medications for Parkinson's disease, such as selegiline or rasagiline
+ Linezolid or methylene blue
Age: If you are 65 years or older, inform your doctor.
Breastfeeding: Do not breastfeed while taking this medication. Inform your doctor if you are breastfeeding or plan to breastfeed.
Pediatric considerations: If your child is a premature baby or newborn, do not give them this medication.

Additional Important Information:

This list is not exhaustive, and it is crucial to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins. Your doctor will help you determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without consulting your doctor.
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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. Before operating a vehicle or engaging in activities that require alertness, wait until you understand how this medication affects you.

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

This medication may increase your susceptibility to sunburn. Exercise caution when exposed to sunlight, and notify your doctor if you experience increased sensitivity to the sun.

It is critical to be aware that overdoses of this medication have occurred in children, which can lead to severe health complications and potentially be fatal. If you have questions or concerns, discuss them with your doctor.

When administering this medication to children, exercise caution and consult with their doctor. If you are pregnant or planning to become pregnant, inform your doctor 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
  • Blurred vision
  • Dry mouth
  • Fixed, dilated pupils
  • Flushed skin
  • Fever
  • Agitation
  • Hallucinations
  • Tremors
  • Convulsions
  • Hypotension
  • Tachycardia
  • Cardiac arrhythmias
  • Respiratory depression

What to Do:

Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is supportive and symptomatic. Gastric lavage may be considered if ingestion is recent. Physostigmine may be used for severe anticholinergic symptoms under strict medical supervision.

Drug Interactions

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Contraindicated Interactions

  • Monoamine Oxidase Inhibitors (MAOIs) (concurrent use or within 14 days of MAOI discontinuation)
  • Patients with narrow-angle glaucoma
  • Patients with prostatic hypertrophy or bladder neck obstruction
  • Patients with stenosing peptic ulcer
  • Patients with symptomatic prostatic hypertrophy
  • Elderly, debilitated patients (due to increased susceptibility to anticholinergic effects)
  • Neonates or premature infants
  • Nursing mothers
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Major Interactions

  • CNS depressants (e.g., alcohol, sedatives, hypnotics, anxiolytics, opioids, other antihistamines): Potentiation of CNS depression.
  • Anticholinergic drugs (e.g., tricyclic antidepressants, atropine, benztropine): Additive anticholinergic effects (dry mouth, blurred vision, urinary retention, constipation).
  • Serotonergic agents (e.g., SSRIs, SNRIs, triptans): Cyproheptadine can antagonize the effects of these drugs, particularly in the context of serotonin syndrome treatment, potentially worsening symptoms if used inappropriately.
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Moderate Interactions

  • Potassium chloride (oral forms): Increased risk of GI lesions due to anticholinergic-induced decreased GI motility.
  • Topical anticholinergics (e.g., scopolamine patches): Additive anticholinergic effects.

Monitoring

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Baseline Monitoring

Allergy symptoms (if for allergies)

Rationale: To establish baseline severity and guide treatment.

Timing: Prior to initiation of therapy.

Weight (if for appetite stimulation)

Rationale: To monitor efficacy of appetite stimulation.

Timing: Prior to initiation of therapy.

Mental status/Cognitive function

Rationale: To assess baseline and monitor for anticholinergic effects, especially in elderly.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Symptom control (allergies or appetite)

Frequency: Regularly during therapy, as clinically indicated.

Target: Reduction in allergy symptoms; weight gain (if for appetite).

Action Threshold: Lack of efficacy or worsening symptoms may require dose adjustment or alternative therapy.

Sedation/Drowsiness

Frequency: Daily, especially during initial therapy or dose changes.

Target: Minimal or tolerable sedation.

Action Threshold: Excessive sedation may require dose reduction or administration at bedtime.

Anticholinergic side effects (dry mouth, blurred vision, urinary retention, constipation)

Frequency: Regularly, as clinically indicated.

Target: Absence or mild, tolerable symptoms.

Action Threshold: Severe or bothersome symptoms may require dose reduction or discontinuation.

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Symptom Monitoring

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

Special Patient Groups

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Pregnancy

Cyproheptadine is classified as 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 and the potential benefits outweigh the potential risks.

Trimester-Specific Risks:

First Trimester: No known increased risk of major birth defects based on limited human data and animal studies.
Second Trimester: No specific risks identified.
Third Trimester: No specific risks identified, but anticholinergic effects could theoretically affect the neonate if used close to delivery.
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Lactation

Cyproheptadine is excreted into breast milk and is contraindicated in nursing mothers due to the potential for serious adverse reactions in the infant (e.g., sedation, irritability, paradoxical excitation) and the potential to decrease milk supply due to anticholinergic effects.

Infant Risk: High (sedation, irritability, paradoxical excitation, potential for decreased milk supply)
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Pediatric Use

Contraindicated in neonates and premature infants. Use with caution in young children due to increased susceptibility to anticholinergic side effects and the potential for paradoxical excitation (restlessness, irritability, insomnia). Not recommended for children under 2 years of age for allergic conditions.

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Geriatric Use

Elderly patients are more susceptible to the anticholinergic side effects (e.g., sedation, confusion, dry mouth, urinary retention, constipation) and paradoxical excitation. Lower doses are generally recommended, and use should be with extreme caution or avoided if possible, especially in those with pre-existing conditions like glaucoma or prostatic hypertrophy.

Clinical Information

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Clinical Pearls

  • Cyproheptadine is one of the few antihistamines with significant antiserotonergic properties, making it useful off-label for the treatment of serotonin syndrome (particularly mild to moderate cases).
  • It is commonly used off-label as an appetite stimulant in various conditions, including cancer cachexia, anorexia nervosa, and in children with poor weight gain.
  • Due to its sedating and anticholinergic effects, it is often dosed at bedtime when used for allergic conditions.
  • Patients should be warned about the potential for significant drowsiness and impaired ability to perform tasks requiring mental alertness.
  • Paradoxical excitation (restlessness, irritability, insomnia) can occur, especially in young children and occasionally in adults.
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Alternative Therapies

  • Other first-generation antihistamines (e.g., Diphenhydramine, Hydroxyzine)
  • Second-generation antihistamines (e.g., Loratadine, Cetirizine, Fexofenadine) for allergic conditions (less sedating)
  • For appetite stimulation: Mirtazapine, Dronabinol, Megestrol acetate (depending on underlying cause)
  • For serotonin syndrome: Benzodiazepines (for agitation/hyperthermia), supportive care
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Cost & Coverage

Average Cost: Typically low cost per 473ml bottle (2mg/5ml)
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (preferred generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it is 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 it's a good idea to check with your pharmacist. If you have any questions or concerns about your medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.