Periactin 4mg Tablets

Manufacturer MERCK HUMAN HEALTH 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 Antihistamine, Serotonin Antagonist
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Pregnancy Category
Category B
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FDA Approved
Jan 1970
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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 and is sometimes used for this purpose. It often causes drowsiness.
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How to Use This Medicine

Taking Your Medication

To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. You can take this medication with or without food. If you experience stomach upset, taking it with food may help.

Storing and Disposing of Your Medication

To maintain the quality and safety of your medication, store it at room temperature in a dry location. Avoid storing it in a bathroom. Keep all medications in a secure place, out of the reach of children and pets, to prevent accidental ingestion or misuse.

What to Do If You Miss a Dose

If you forget to take a dose, take it as soon as you remember. However, if it's almost 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 a missed one.
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Lifestyle & Tips

  • Avoid driving or operating heavy machinery until you know how this medication affects you, as it can cause significant drowsiness.
  • Avoid alcohol and other medications that cause drowsiness, as this can worsen the sedative effects.
  • To relieve dry mouth, suck on sugarless candy or ice chips, or use artificial saliva.
  • Take with food or milk if stomach upset occurs.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: 4 mg orally three times a day
Dose Range: 4 - 20 mg

Condition-Specific Dosing:

allergies: 4 mg orally three times a day; range 4-20 mg/day, max 0.5 mg/kg/day
appetite_stimulation: 4 mg orally three times a day, may be increased gradually to 16 mg/day
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Pediatric Dosing

Neonatal: Not established
Infant: Not established (contraindicated in neonates/premature infants)
Child: 0.25 mg/kg/day or 8 mg/m2/day in 2-3 divided doses (for allergies, 2-6 years: 2 mg twice or three times a day; 7-14 years: 4 mg twice or three times a day)
Adolescent: 4 mg orally three times a day (similar to adult dosing for allergies)
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Dose Adjustments

Renal Impairment:

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

Hepatic Impairment:

Mild: Use with caution
Moderate: Use with caution, consider lower doses due to extensive hepatic metabolism
Severe: Contraindicated or use with extreme caution; significant dose reduction likely required

Pharmacology

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Mechanism of Action

Cyproheptadine is a first-generation antihistamine that competitively antagonizes H1-histamine receptors, thereby preventing histamine's effects on capillaries, bronchi, and GI smooth muscle. It also possesses significant antiserotonergic activity (5-HT2 receptor antagonism) and anticholinergic properties. Its appetite stimulant effect is thought to be related to its serotonin antagonism.
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Pharmacokinetics

Absorption:

Bioavailability: Well absorbed orally, but specific percentage not widely reported.
Tmax: 6-9 hours
FoodEffect: Food may slightly delay absorption but does not significantly affect bioavailability.

Distribution:

Vd: Not precisely quantified, but widely distributed throughout the body.
ProteinBinding: Highly protein bound (approximately 96%)
CnssPenetration: Yes (readily crosses the blood-brain barrier, contributing to sedative effects)

Elimination:

HalfLife: Approximately 8 hours (range 5-9 hours)
Clearance: Not precisely quantified, but primarily hepatic.
ExcretionRoute: Mainly renal (approximately 40% of dose excreted in urine, primarily as metabolites); approximately 2-20% excreted in feces.
Unchanged: Very little unchanged drug excreted in urine.
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Pharmacodynamics

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

Safety & Warnings

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Side Effects

Serious 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 notice 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
Changes in menstrual periods

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
Fatigue
Weakness
Headache
Constipation
Diarrhea
Stomach pain
Upset stomach
Vomiting
Decreased appetite
Increased appetite
Weight gain
Dry mouth
Dry nose
Stuffy nose
Nervousness
Restlessness
Shakiness
Sleep disturbances

Reporting Side Effects

If you have questions or concerns about side effects, 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
  • Confusion or disorientation
  • Difficulty urinating
  • Severe constipation
  • Blurred vision or eye pain
  • Fast or irregular heartbeat
  • Unusual excitement or nervousness (especially in children)
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Before Using This Medicine

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

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

If you have a known allergy to cyproheptadine or any component of this medication. Describe your allergic reaction, including any 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 understand how this drug affects you, avoid operating a vehicle and engaging in other activities that require your full attention.

This medication may interfere with the results of allergy skin tests, so be sure to notify your doctor and laboratory personnel that you are taking it. Before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that can cause drowsiness, consult with your doctor.

You may be more susceptible to sunburn while taking this medication, so exercise caution when spending time outdoors. If you experience increased sensitivity to the sun, notify your doctor. It is crucial 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 any questions or concerns, discuss them with your doctor.

This medication should be used with caution in children, and it is recommended that you consult with your doctor. If you are pregnant or planning to become pregnant, you will need to discuss the potential benefits and risks of taking this medication during pregnancy with your doctor.
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Overdose Information

Overdose Symptoms:

  • Severe drowsiness or deep sleep
  • Dizziness
  • Ataxia (loss of coordination)
  • Weakness
  • Tinnitus (ringing in ears)
  • Blurred vision
  • Dilated pupils
  • Dry mouth and skin
  • Flushing
  • Fever
  • Agitation
  • Hallucinations
  • Tremors
  • Convulsions
  • Hypotension
  • Coma
  • Cardiorespiratory collapse

What to Do:

In case of suspected overdose, seek immediate medical attention. Call 911 or your local poison control center (e.g., 1-800-222-1222 in the US). Treatment is supportive and symptomatic; activated charcoal may be considered if ingested recently. Do NOT induce vomiting.

Drug Interactions

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Contraindicated Interactions

  • Monoamine Oxidase Inhibitors (MAOIs) (concurrent use or within 14 days of MAOI discontinuation)
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Major Interactions

  • CNS depressants (e.g., alcohol, sedatives, hypnotics, anxiolytics, opioids, tricyclic antidepressants, other antihistamines)
  • Anticholinergic drugs (e.g., atropine, scopolamine, tricyclic antidepressants, phenothiazines)
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Moderate Interactions

  • Potassium chloride (wax matrix formulations - increased risk of GI lesions)
  • Topical anesthetics (additive anticholinergic effects)

Monitoring

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Baseline Monitoring

Patient history (glaucoma, prostatic hypertrophy, urinary retention, asthma)

Rationale: To identify contraindications or conditions requiring caution due to anticholinergic effects.

Timing: Prior to initiation

Liver function tests (LFTs)

Rationale: Cyproheptadine is extensively metabolized by the liver; baseline assessment is prudent, especially in patients with suspected hepatic impairment.

Timing: Prior to initiation (if clinically indicated)

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Routine Monitoring

Sedation/Drowsiness

Frequency: Daily, especially during initial therapy or dose adjustments

Target: Minimal to tolerable levels

Action Threshold: Excessive drowsiness interfering with daily activities; consider dose reduction or alternative.

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

Frequency: Daily

Target: Minimal to tolerable levels

Action Threshold: Severe or bothersome symptoms; consider dose reduction or symptomatic management.

Weight (if used for appetite stimulation)

Frequency: Weekly to monthly

Target: Desired weight gain

Action Threshold: Lack of desired weight gain after adequate trial, or excessive/unintended weight gain.

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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

Category B. Animal studies have not shown harm, but human studies are limited. Use only if clearly needed.

Trimester-Specific Risks:

First Trimester: Limited data, but generally considered low risk based on animal data.
Second Trimester: Limited data, generally considered low risk.
Third Trimester: Limited data, generally considered low risk. Antihistamines close to term theoretically could cause withdrawal symptoms in neonates, but specific data for cyproheptadine is lacking.
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Lactation

L3 (Moderately safe). Cyproheptadine is excreted in breast milk. Due to potential for sedation and anticholinergic effects in the infant, and potential to decrease milk supply, use with caution. Observe infant for drowsiness or irritability.

Infant Risk: Moderate risk of sedation, irritability, or anticholinergic effects (e.g., dry mouth, constipation). Potential for decreased milk supply.
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Pediatric Use

Contraindicated in neonates and premature infants. Use with caution in children, especially those under 2 years, due to increased susceptibility to paradoxical excitation (restlessness, irritability) or convulsions. Dosing must be carefully calculated by weight/surface area.

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Geriatric Use

Increased susceptibility to anticholinergic side effects (e.g., dry mouth, urinary retention, constipation, blurred vision) and CNS effects (e.g., sedation, dizziness, confusion). Use lower initial doses and titrate carefully. Avoid in elderly patients with conditions exacerbated by anticholinergic effects (e.g., glaucoma, prostatic hypertrophy). The Beers Criteria recommend avoiding first-generation antihistamines in older adults due to high anticholinergic activity and risk of sedation and falls.

Clinical Information

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Clinical Pearls

  • Cyproheptadine is a potent first-generation antihistamine with significant sedative and anticholinergic effects. Warn patients about impaired ability to drive or operate machinery.
  • Its appetite stimulant effect is unique among antihistamines and is often utilized off-label for weight gain in various conditions (e.g., cancer cachexia, anorexia nervosa, or in children with poor appetite).
  • Paradoxical excitation (restlessness, nervousness, insomnia) can occur, especially in young children or elderly patients, rather than sedation.
  • Patients should avoid alcohol and other CNS depressants while taking cyproheptadine.
  • Due to its anticholinergic properties, it should be used with caution or avoided in patients with narrow-angle glaucoma, prostatic hypertrophy, or bladder neck obstruction.
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Alternative Therapies

  • Second-generation antihistamines (e.g., loratadine, cetirizine, fexofenadine) for allergies (less sedating, less anticholinergic)
  • Other appetite stimulants (e.g., dronabinol, megestrol acetate, mirtazapine - depending on underlying cause of appetite loss)
  • Other first-generation antihistamines (e.g., diphenhydramine, chlorpheniramine) for allergy relief (similar side effect profile)
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Cost & Coverage

Average Cost: $10 - $30 per 30 tablets (4mg)
Generic Available: Yes
Insurance Coverage: Tier 1 or 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 promptly. To ensure safe and effective treatment, 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 for more information. If you have any questions or concerns about this 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 emergency medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.