Apigrane
Apigrane Uses, Dosage, Side Effects, Food Interaction and all others data.
Apigrane binds with high affinity to human cloned 5-HT1B/1D receptors. Apigrane presumably exerts its therapeutic effects in the treatment of migraine and cluster headaches through agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels and sensory nerves of the trigeminal system, which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
Apigrane constricts cranial blood vessels and prevents the release of vasoactive peptides. The dose of sumatriptan varies widely by route of administration and in most cases, no more than 2 doses should be given daily. Medication overuse headaches may occur in patients who use sumatriptan frequently.
| Trade Name | Apigrane |
| Availability | Prescription only |
| Generic | Sumatriptan |
| Sumatriptan Other Names | Sumatriptan, Sumatriptán, Sumatriptanum |
| Related Drugs | Ubrelvy, Botox, prednisone, diclofenac, celecoxib, metoclopramide, verapamil, indomethacin, Imitrex, Reglan |
| Type | |
| Formula | C14H21N3O2S |
| Weight | Average: 295.4 Monoisotopic: 295.135447621 |
| Protein binding | Sumatriptan is 14%-21% bound to protein in circulation. |
| Groups | Approved, Investigational |
| Therapeutic Class | 5-HT Agonists |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Apigrane Succinate is used for adults for the acute treatment of migraine (with or without aura), and the acute treatment of cluster headache.
Apigrane is also used to associated treatment for these conditions: Acute Migraine, Acute Cluster headaches
How Apigrane works
Apigrane is an agonist of 5-HT1B and 5-HT1D. This agonism leads to constriction of cranial blood vessels and inhibits the release of pro-inflammatory neuropeptides. Apigrane decreases carotid arterial blood flow, but increases blood flow velocity in the internal carotid artery and middle cerebral artery.
Dosage
Apigrane dosage
Migraine: 50-100 mg repeated at 2-hr intervals if migraine recurs. Max: 300 mg/24 hr.
Take thismedicationbymouthwith or without food as directed by your doctor, at the first sign of amigraine. The dosage is based on your medical condition and response to treatment. If there is no improvement in your symptoms, do not take more doses of this medication before talking to your doctor. If your symptoms are only partly relieved, or if yourheadachecomes back, you may take another dose at least two hours after the first dose. Do not take more than 200 milligrams in a 24-hour period.
If you are using drugs formigraineattacks on 10 or more days each month, the drugs may actually make yourheadachesworse (medication overuseheadache). Do not usemedicationsmore often or for longer than directed. Tell your doctor if you need to use this medication more often, or if the medication is not working as well, or if yourheadachesget worse.
Side Effects
Transient hypertension, hypotension, dizziness, flushing, fatigue, drowsiness, weakness, seizures, nausea and vomiting, heat, tightness in any part of body, paraesthesia, seizures, inj site reactions, irritation of nasal mucosa and epistaxis. Rebound headache with frequent use.
Toxicity
Symptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation. Overdoses may be fatal and patients should be monitored for 3-5 half lives or while symptoms persist.
Precaution
Conditions predisposing to seizures, presence of coronary risk factors, cardiac arrhythmias, renal or hepatic impairment, elderly, pregnancy, lactation.
Interaction
Concurrent use increased risk of vasospastic reaction with ergotamine and related compounds.
Food Interaction
- Avoid excessive or chronic alcohol consumption. Alcohol increased the risk of GI bleeding, ulcer, and perforation when taken with sumatriptan.
- Take with or without food.
Apigrane Cholesterol interaction
[Major] The group of drugs known as 5-hydroxytryptamine1 receptor (5-HT1) agonists can cause vasospastic reactions, including coronary vasospasm, peripheral vascular ischemia, and colonic ischemia.
Rarely, serious adverse cardiac events including acute myocardial infarction, arrhythmia, cardiac arrest, and death have been reported within a few hours following the administration of 5-HT1 agonists, in some cases even in patients with no prior history or findings of coronary artery disease (CAD).
Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension, as have transient increases in blood pressure and peripheral vascular resistance.
In general, patients with potentially unrecognized CAD as predicted by the presence of risk factors (e.g., hypertension, hypercholesterolemia, tobacco use, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, or male over 40 years of age) should not be administered 5-HT1 agonists unless a cardiovascular evaluation provides satisfactory clinical evidence indicating the lack of CAD, ischemic heart disease, or other significant underlying cardiovascular disease.
As a precaution, the manufacturers recommend that the first dose be administered under medical surveillance in such patients, and that electrocardiographic monitoring be considered during the interval immediately following administration to help detect any asymptomatic cardiac ischemia that may occur.
Periodic cardiovascular evaluations should be performed during intermittent, long-term use.
Apigrane Drug Interaction
Major: duloxetine, cyclobenzaprine, ondansetron, sertralineModerate: acetaminophen / hydrocodoneUnknown: amphetamine / dextroamphetamine, diphenhydramine, omega-3 polyunsaturated fatty acids, fluticasone nasal, pregabalin, albuterol, montelukast, levothyroxine, topiramate, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, alprazolam, cetirizine
Apigrane Disease Interaction
Major: CAD risk factors, cardiovascular disease, liver diseaseModerate: seizure disorders
Volume of Distribution
Apigrane has a volume of distribution of 50±8L for a 6mg subcutaneous dose, or 2.7L/kg.
Elimination Route
A 6mg subcutaneous injection of sumatriptan reaches a Cmax of 69.5ng/mL (95% CI of 62.8-76.9ng/mL) with a Tmax of 0.17h (95% CI of 0.08-0.33h), an AUC of 9.0h*ng/mL (95% CI of 7.5-10.9h*ng/mL), and a bioavailability of 100%.
A 25mg oral dose of sumatriptan reaches a Cmax of 16.5ng/mL (95% CI of 13.5-20.1ng/mL) with a Tmax of 1.50h (95% CI of 0.50-2.00h), an AUC of 8.7h*ng/mL (95% CI of 6.1-12.5h*ng/mL), and a bioavailability of 14.3% (95% CI of 11.4-17.9%).
A 20mg intranasal dose of sumatriptan reaches a Cmax of 12.9ng/mL (95% CI of 10.5-15.9ng/mL) with a Tmax of 1.50h (95% CI of 0.25-3.00h), an AUC of 7.4h*ng/mL (95% CI of 5.0-10.8h*ng/mL), and a bioavailability of 15.8% (95% CI of 12.6-19.8%).
A 25mg rectal dose of sumatriptan reaches a Cmax of 22.9ng/mL (95% CI of 18.4-28.6ng/mL) with a Tmax of 1.00h (95% CI of 0.75-3.00h), an AUC of 14.6h*ng/mL (95% CI of 11.3-18.8h*ng/mL), and a bioavailability of 19.2% (95% CI of 15.3-24.1%).
Half Life
Subcutaneous sumatriptan has a half life of 1.9h (95% CI of 1.7-2.0h). Oral sumatriptan has a half life of 1.7h (95% CI of 1.4-1.9h). Rectal sumatriptan has a half life of 1.8h (95% CI of 1.6-2.2h). Intrsnasal sumatriptan has a half life of 1.8h (95% CI of 1.7-2.0h).
Clearance
Subcutaneous sumatriptan has a clearance of 0.22L/min (95% CI of 0.19-0.25L/min). Oral sumatriptan has a clearance of 0.17L/min (95% CI of 0.14-0.21L/min). Rectal sumatriptan has a clearance of 0.17L/min (95% CI of 0.14-0.21L/min). Intrsnasal sumatriptan has a clearance of 0.21L/min (95% CI of 0.18-0.25L/min). Total plasma clearance of sumatriptan is approximately 1200mL/min.
Elimination Route
22±4% is excreted in the urine as unchanged sumatriptan and 38±7% in urine as indole acetic acid approximately 40% is excreted in the feces.
Pregnancy & Breastfeeding use
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindication
Not to be used prophylactically and in patients with basilar or hemiplegic or ophthalmoplegic migraine. History of MI or stroke, severe hepatic impairment, ischaemic heart disease, uncontrolled hypertension, peripheral vascular disease, hypersensitivity to sulfonamides.
Innovators Monograph
You find simplified version here Apigrane
Apigrane contains Sumatriptan see full prescribing information from innovator Apigrane Monograph, Apigrane MSDS, Apigrane FDA label
FAQ
What is Apigrane used for?
Apigrane is used to treat migraine or cluster headaches once the pain has started, but there are other medicines available that may help to reduce the number and frequency of attacks.
How safe is Apigrane?
Taking too much Apigrane may make you very ill. An overdose can cause fainting, slowed heart rate, vomiting, loss of bladder and bowel control, and sleepiness. It can narrow your blood vessels leading to heart problems such as chest pains, abnormal heart rhythm or a heart attack.
How does Apigrane work?
Apigrane works on the serotonin receptors located on blood vessels in your brain. This causes them to narrow. This helps take away the headache and eases other symptoms such as feeling or being sick and sensitivity to light and sound.
What are the common side effects of Apigrane?
Common side effects of Apigrane are include :
- flushing
- tingling feeling
- feeling warm or cold
- drowsiness
- tiredness
- weakness
- dizziness
- upset stomach
- diarrhea
- nausea
- muscle cramps
Is Apigrane safe during pregnancy?
Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
Apigrane should only be given during pregnancy when benefit outweighs risk.
Is Apigrane safe during breastfeeding?
Apigrane is considered compatible with breastfeeding, as minimal amounts are excreted into milk.
Can I drink alcohol with Apigrane?
Alcohol does not affect how Apigrane works. However, it's best not to drink alcohol during a headache attack. Migraines and cluster headaches can sometimes be triggered by alcohol.
Can I drive after taking Apigrane?
Use Apigrane as soon as the migraine headache or cluster headache develops. It can make you feel tired or sleepy. If this happens, do not drive and do not use tools or machines.
When Is the best taken of Apigrane?
Take Apigrane as soon as a migraine or cluster headache starts. The tablets usually work within 30 to 60 minutes. The spray and injection work quicker.
How many hours does Apigrane last?
Apigrane is a short-acting medication with a half-life of around two hours. A Apigrane dose will be completely cleared from the body in 10 hours.
Should Apigrane be taken on an empty stomach?
Swallow the tablet whole with water or other liquids. Do not crush, break, or chew it. You may take the tablet with or without food.
Does Apigrane make me sleep?
Use Apigrane as soon as the migraine headache or cluster headache develops. It can make you feel tired or sleepy.
What does Apigrane feel like?
feeling warm or cold. tingling or prickling sensations in your skin. pressure or pain in your chest, neck, jaw, or throat.
Does Apigrane cause weight loss?
Weight loss isn't a direct side effect of Apigrane.
Is Apigrane hard on the kidneys?
The effect of reduced kidney function on how Apigrane acts in the body has not been evaluated. Apigrane is not recommended for use if you have reduced kidney function.
Is Apigrane a sedative?
Apigrane can cause adverse central nervous system events outside migraine attacks. It can cause mild sedative effects such as sleepiness or fatigue.
Will Apigrane affect my fertility?
There's no firm evidence that Apigrane affects fertility in men or women.
Can Apigrane cause a miscarriage?
Three small studies do not suggest taking Apigrane in early pregnancy is linked to miscarriag.
Who should not take Apigrane?
People who have ever had a stroke or mini stroke,people with very high or uncontrolled high blood pressure,people with severe liver problems they should not take Apigrane.
What happens if I miss a dose?
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
Can I overdose on Apigrane?
Taking too much Apigrane may make you very ill. An overdose can cause fainting, slowed heart rate, vomiting, loss of bladder and bowel control, and sleepiness.
