sumatriptan intranasal

Action and Spectrum

Actions and spectrum: 

• Serotonin (5-HT1B/1D) Receptor Agonism: sumatriptan acts as an agonist (activator) of serotonin receptors, specifically the 5-HT1B and 5-HT1D receptors. Activation of these receptors leads to several effects: 
• a. Vasoconstriction: sumatriptan causes constriction of blood vessels in the brain. This helps alleviate the dilation of blood vessels that occurs during a migraine attack, which is believed to be involved in the pathophysiology of migraines. 
• b. Inhibition of Neurogenic Inflammation: sumatriptan inhibits the release of inflammatory neuropeptides from trigeminal nerves, which play a role in migraine pain and neurogenic inflammation. 
• Relief of Migraine Symptoms: sumatriptan intranasal formulation provides rapid relief from various migraine symptoms, including headache, vomiting, nausea, and sensitivity to sound and light. 

The spectrum of sumatriptan intranasal refers to its effectiveness in treating migraine attacks. sumatriptan has been shown to be effective in the treatment of acute migraines, providing relief from headache and associated symptoms when administered intranasally. However, it is important to note that sumatriptan is not a preventive medication for migraines and should be used specifically during an acute migraine episode. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Throat discomfort (0.8-2.4%) 

Burning sensation (0.4-1.4%) 

discomfort /disorder of nasal sinuses/cavity (2.5-3.8%) 

Vertigo/Dizziness (1-1.7%)  

>10% 

Gastrointestinal: vomiting/nausea (11-13.5%) 

unusual/Bad taste (13.5-24.5%)  

Frequency not defined 

Cardiovascular:  hypertension, tachycardia, Flushing, palpations, edema, arrhythmia 

ear infections, disturbance of hearing 

visual disturbances, Eye irritation 

Gastrointestinal: diarrhea, GERD, thirst, Abdominal discomfort, dysphagia, dry mouth 

Neurological: anxiety, tremors, chills, agitation, Drowsiness/sedation, sleep disturbances, syncope, depression, confusion 

Skin: pruritus, skin rash or eruption, erythema 

Atypical Sensations: numbness, cold sensation, Tingling, pressure sensation, feeling of tightness 

tightness of Chest/discomfort, chest heaviness/pressure 

Musculoskeletal: backache, joint symptoms, myalgia, Neck pain/stiffness, weakness, arthritis, muscle cramps 

Respiratory: lower respiratory infection, Dyspnea 

Urogenital: dysmenorrhea, Dysuria  

Post marketing Reports 

Cardiovascular:  cardiomyopathy, Prinzmetal variant angina, shock, Atrial fibrillation, colonic ischemia, pulmonary embolism 

Eye: retinal artery occlusion, loss of vision, Ischemic optic neuropathy, retinal vein thrombosis 

Hepatic: Elevated LFTs 

Psychiatric: Panic disorder 

Skin: hypersensitivity reactions, exacerbation of sunburn 

Nonspecific: cyanosis, death, Angioneurotic edema, temporal arteritis 

Blood: pancytopenia, Hemolytic anemia, thrombocytopenia 

Ear, throat, nose: Deafness 

Gastrointestinal: dry mouth, Ischemic colitis 

Neurological: cerebrovascular accident, serotonin syndrome, CNS vasculitis, dysphasia, subarachnoid hemorrhage 

Respiratory: bronchospasm 

Urogenital: acute renal failure 

Black Box Warning

Black Box Warning: 

There is no specific black box warning for sumatriptan intranasal. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: sumatriptan intranasal is contraindicated in individuals with a known hypersensitivity or allergy to sumatriptan or any of its components. Allergic reactions to sumatriptan can range from mild symptoms to severe, potentially life-threatening reactions. 
• Ischemic Heart Disease: sumatriptan intranasal is contraindicated in patients with a history of ischemic heart disease, including angina, heart attack, or coronary artery vasospasm. It should not be used in individuals with a history of significant cardiovascular conditions. 
• Uncontrolled Hypertension: sumatriptan intranasal should not be used in individuals with uncontrolled hypertension (high blood pressure) because it can further increase blood pressure. Blood pressure should be well-controlled before initiating treatment with sumatriptan. 
• Hemiplegic or Basilar Migraine: sumatriptan intranasal is contraindicated in patients with hemiplegic migraine or basilar migraine, as these conditions may have similar symptoms to other serious neurological conditions. Using sumatriptan in such cases could potentially worsen these conditions. 
• Within 24 Hours of Other Triptans or Ergotamine Derivatives: Concomitant use of sumatriptan intranasal with other triptans or ergotamine derivatives is contraindicated. Using these medications within 24 hours of each other can increase the risk of developing serotonin syndrome, a potentially life-threatening condition. 

Caution: 

• Cardiovascular Risk Factors: Individuals with cardiovascular risk factors like high blood pressure, diabetes, smoking, obesity, or family history of cardiovascular disease, should use sumatriptan intranasal with caution. The medication may have vasoconstrictive effects on blood vessels, and it is important to monitor cardiovascular function during treatment. 
• Peripheral Vascular Disease: sumatriptan intranasal should be used with caution in individuals with peripheral vascular disease (circulatory disorders affecting the blood vessels outside the heart and brain) because of the potential for vasoconstriction. 
• Impaired Renal or hepatic Function: Patients with impaired liver or kidney function may have reduced clearance of sumatriptan, and caution should be exercised when using sumatriptan intranasal in these individuals.  
• Seizure Disorders: sumatriptan intranasal should be used with caution in patients with a history of seizures or epilepsy. The medication may lower the seizure threshold, although seizures are rare. 
• Serotonin Syndrome: sumatriptan, like other triptans, can cause serotonin syndrome that increase serotonin levels. Caution should be exercised when using sumatriptan intranasal in combination with these medications. 
• Pregnancy and Lactation: The use of sumatriptan intranasal during pregnancy and lactation should be approached with caution.

Comorbidities: 

• Cardiovascular Disease: Individuals with cardiovascular disease, including coronary artery disease, angina, previous heart attack, or uncontrolled hypertension, should use sumatriptan intranasal with caution. sumatriptan can cause vasoconstriction, potentially affecting blood flow to the heart and increasing blood pressure. 
• Stroke or Transient Ischemic Attack (TIA): sumatriptan intranasal should be used with caution in individuals with a history of stroke or transient ischemic attack. The vasoconstrictive effects of sumatriptan may pose a risk in individuals with compromised cerebral blood flow. 
• Peripheral Vascular Disease: Individuals with peripheral vascular disease, which involves circulatory disorders affecting the blood vessels outside the heart and brain, should use sumatriptan intranasal with caution. Vasoconstriction associated with sumatriptan may exacerbate the condition. 
• Liver or Kidney Impairment: Patients with impaired liver or kidney function may require caution when using sumatriptan intranasal. Dose adjustments or alternative treatment options may be necessary in these cases, as clearance of the medication may be reduced. 
• Epilepsy or Seizure Disorders: sumatriptan intranasal should be used with caution in individuals with a history of epilepsy or seizure disorders. Although seizures are rare, sumatriptan has the potential to lower the seizure threshold. 
• Serotonin Syndrome Risk: Combining sumatriptan intranasal with other medications that increase serotonin levels (such as selective serotonin reuptake inhibitors or serotonin-norepinephrine reuptake inhibitors) may increase the risk of serotonin syndrome. Caution should be exercised in such situations. 

Pregnancy / Lactation

Pregnancy consideration: US FDA pregnancy category: C 

Lactation: Excreted into human milk: Yes  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• 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 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: 

sumatriptan is a medication that belongs to the class of drugs known as triptans. It is used for the acute treatment of migraines and cluster headaches. sumatriptan acts primarily as an agonist (activator) of serotonin 5-HT1B and 5-HT1D receptors, which are located on intracranial blood vessels and nerve terminals. Activation of these receptors leads to vasoconstriction (narrowing of blood vessels) and inhibition of neurogenic inflammation, thereby relieving migraine headaches.  

Pharmacodynamics: 

• Activation of Serotonin Receptors: sumatriptan acts as an agonist (activator) at serotonin (5-HT1B/1D) receptors located on blood vessels and nerve terminals in the brain. 
• Vasoconstriction: sumatriptan causes the constriction of blood vessels (vasoconstriction) in the brain and surrounding tissues. This effect is particularly significant in the intracranial blood vessels, helping to reverse the dilation of blood vessels during a migraine attack. Vasoconstriction helps reduce inflammation and alleviate the pain associated with migraines. 
• Inhibition of Neurogenic Inflammation: sumatriptan inhibits the release of inflammatory neuropeptides, such as substance P, from nerve endings in the trigeminal system. These neuropeptides play a role in transmitting pain signals and promoting neurogenic inflammation during migraines. By inhibiting their release, sumatriptan helps reduce the inflammation and associated symptoms. 
• Central Nervous System Effects: sumatriptan modulates neuronal activity in the central nervous system (CNS), particularly within the trigeminal pain pathway. It inhibits the release of pain mediators and reduces the transmission of pain signals within the CNS, leading to pain relief during migraines. 

Pharmacokinetics: 

Absorption 

When sumatriptan is administered intranasally, it is absorbed through the nasal mucosa and enters the systemic circulation. Intranasal administration allows for rapid absorption due to the rich vascular supply in the nasal mucosa. 

Distribution 

sumatriptan is distributed throughout the body, including the brain and peripheral tissues. It crosses blood-brain barrier and reaches the target sites in the brain, where it has therapeutic effects on migraines. 

Metabolism 

sumatriptan undergoes extensive metabolism in the liver. The primary metabolic pathway involves oxidation via the cytochrome P450 enzyme system, specifically the CYP3A4 and CYP2D6 enzymes. The metabolites formed are inactive. The metabolism of sumatriptan can vary among individuals due to genetic variations in the enzymes involved. 

Elimination and excretion 

The metabolites of sumatriptan, as well as a small portion of unchanged drug, are primarily excreted in the urine. The elimination half-life is approximately 2 hours, indicating that it is rapidly cleared from the body. 

Adminstartion

Administration: 

• Preparation: Before using sumatriptan intranasal, carefully read and the medication package insert. Ensure that the medication is not expired. 
• Positioning: Sit or stand upright in a comfortable position. 
• Prime the Device: Before the first use, or if the device has not been used for a certain period as specified in the instructions, prime the device according to the manufacturer’s instructions. Priming ensures that the medication is dispensed properly. 
• Insert the Nozzle: Gently insert the nozzle of the device into one nostril until it stops. 
• Breath Control: Close the other nostril by pressing with finger, and tilt head slightly forward to ensure proper delivery of the medication. Breathe gently through your mouth. 
• Actuate the Device: Activate the device as per the instructions provided, which may involve pressing a button or plunger. This will release a dose of sumatriptan into the nostril. 
• Sniff: Inhale gently and steadily through your nose to ensure the medication reaches the nasal passages. Avoid sniffing forcefully or inhaling through the device. 
• Repeat for the Other Nostril: If instructed to take a second dose, repeat the process for the other nostril using a new device. 
• Post-Administration: After using sumatriptan intranasal, remove the device from your nostril and discard it properly, according to the instructions or local regulations. Do not reuse the device. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: sumatriptan intranasal 

Pronounced: (Soo-ma-TRIP-tan in-truh-NAZE-ul)  

Why do we use sumatriptan intranasal? 

• Migraine Relief: sumatriptan intranasal is effective in providing relief from the acute symptoms of migraines, including headache pain, nausea, sensitivity to light (photophobia), and sensitivity to sound (phonophobia). 
• Rapid Onset of Action: One of the advantages of using sumatriptan intranasal is its rapid onset of action. It is designed to be absorbed quickly through the nasal mucosa, leading to a faster response compared to oral medications. 
• Convenience and Ease of Use: The intranasal formulation of sumatriptan offers a convenient and user-friendly method of administration.