cyproheptadine

Action and Spectrum

Actions and Spectrum: 

Its actions include: 

• Blocking the effects of histamine, a chemical messenger involved in allergic reactions. This helps to reduce symptoms such as itching, sneezing, and runny nose. 
• Acting as a serotonin antagonist, which means it blocks the effects of serotonin, another chemical messenger in the brain. This can help to reduce the severity of migraines and other headaches. 
• Stimulating appetite and promoting weight gain, which makes it useful for treating conditions such as anorexia and cachexia. 

The spectrum of cyproheptadine includes a wide range of conditions that it can be used to treat, including: 

• Allergic reactions, such as hay fever, urticaria, and allergic rhinitis 
• Migraines and other headaches 
• Insomnia and other sleep disorders 
• Anorexia and cachexia 
• Irritable bowel syndrome 
• Serotonin syndrome 
• Post-traumatic stress disorder 
• Anxiety and depression. 

Drug Interaction

Adverse Reaction

Frequency Not Defined  

Drowsiness  

Lassitude  

Dizziness  

Disturbed coordination  

Restlessness  

CNS depression  

Less commonly  

Insomnia  

Seizures  

Tremors  

Toxic psychosis  

Palpitation  

Paresthesia  

Tachycardia  

Hypotension  

Palpitation  

Black Box Warning

Black Box Warning 

The black box warning for cyproheptadine states that the drug can cause a potentially fatal condition called serotonin syndrome when used in combination with certain antidepressants, such as selective serotonin reuptake inhibitors (SSRIs) or monoamine oxidase inhibitors (MAOIs). 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• cyproheptadine is contraindicated in patients with a known hypersensitivity to the medication. 
• It is also contraindicated in patients with severe liver or kidney disease, as well as in those with a history of angle-closure glaucoma or urinary retention. 

Cautions: 

• cyproheptadine may cause drowsiness, so patients should avoid activities that require alertness, such as driving or operating heavy machinery. 
• It may also cause dry mouth, so patients should drink plenty of water and avoid alcohol. 
• cyproheptadine may interact with other medications, such as antidepressants, so patients should inform their healthcare provider of all medications they are taking before starting treatment. 
• It should be used with caution in patients with a history of cardiovascular disease or hypertension, as it may cause an increase in blood pressure. 
• Patients should also be monitored for potential side effects, such as weight gain, changes in appetite, or gastrointestinal symptoms. 

Pregnancy / Lactation

Pregnancy warnings:     

US FDA pregnancy category: B 

Lactation:   

Excreted into human milk is unknown  

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

cyproheptadine is an antihistamine and serotonin antagonist medication that is used to treat a variety of conditions, including allergic reactions, migraines, and insomnia. 

Pharmacodynamics: 

The mechanism of action of cyproheptadine is primarily through its antihistamine properties, which work by blocking the action of histamine, a chemical that is released by the body during an allergic reaction. By blocking the action of histamine, cyproheptadine can reduce symptoms such as sneezing, itching, and runny nose. 

Pharmacokinetics:  

Absorption  

cyproheptadine is rapidly and well absorbed after oral administration, with peak plasma concentrations occurring within 1-2 hours  

Distribution  

cyproheptadine is widely distributed throughout the body, including the brain and other organs. It has a large volume of distribution, which suggests that it is highly protein-bound in plasma.  

Metabolism  

cyproheptadine is metabolized in the liver by the enzyme CYP3A4  

Elimination and excretion  

cyproheptadine is eliminated primarily by the liver and is excreted in the urine and feces. The half-life of the drug is approximately 12 hours, which means that it remains active in the body for a relatively long period of time.

Adminstartion

Administration:  

Oral Administration  

cyproheptadine is a medication that is typically administered orally in the form of a tablet or syrup. The dosage and frequency of administration will depend on the condition being treated and the individual patient’s response to the medication. 

For the treatment of allergic reactions, the usual adult dosage is 4 mg three or four times a day. For the treatment of migraines, the usual adult dosage is 4 mg twice a day. For the treatment of serotonin syndrome, the usual adult dosage is 12 mg per day in divided doses. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: cyproheptadine 

Why do we use cyproheptadine? 

cyproheptadine is a medication that is primarily used to treat allergic reactions, migraines, and serotonin syndrome. 

• Allergic reactions: cyproheptadine is an antihistamine that blocks the action of histamine, a chemical that is released in response to an allergen. This helps to reduce symptoms such as itching, sneezing, runny nose, and watery eyes. 
• Migraines: cyproheptadine has been found to be effective in the prevention of migraines. It works by blocking the action of serotonin, a chemical that is thought to play a role in the development of migraines. 
• Serotonin syndrome: Serotonin syndrome is a serious condition that can occur when there is too much serotonin in the body. cyproheptadine works by blocking the action of serotonin, which helps to reduce the symptoms of serotonin syndrome, such as agitation, confusion, hallucinations, and muscle rigidity