Apremig ODT Dispersible Tablet

Apremig ODT is a calcitonin gene-related peptide receptor antagonist indicated for the acute treatment of migraine with or without aura in adults & preventive treatment of episodic migraine in adults.

The currently accepted theory of migraine pathophysiology considers dysfunction of the central nervous system, in particular the trigeminal ganglion, to be the root cause behind the condition. Activation of the trigeminal ganglion triggers the stimulation of trigeminal afferents that project to the spinal cord and synapse on various pain-sensing intra- and extracranial structures, such as the dura mater. Pain signals are then further transmitted via second-order ascending neurons to the brainstem, hypothalamus, and thalamic nuclei, and from there to several cortical regions (e.g. auditory, visual, motor cortices). The trigeminal ganglion appears to amplify and perpetuate the migraine headache pain through the activation of perivascular fibers and the release of molecules involved in pain generation, such as calcitonin gene-related peptide (CGRP).

The α-isoform of CGRP, expressed in primary sensory neurons, is a potent vasodilator and has been implicated in migraine pathogenesis - CGRP levels are acutely elevated during migraine attacks, return to normal following treatment with triptan medications, and intravenous infusions of CGRP have been shown to trigger migraine-like headaches in migraine patients. In addition to its vasodilatory properties, CGRP appears to be a pronociceptive factor that modulates neuronal excitability to facilitate pain responses.

Rimegepant is an antagonist of the calcitonin gene-related peptide receptor- it competes with CGRP for occupancy at these receptors, preventing the actions of CGRP and its ability to amplify and perpetuate migraine headache pain, ultimately terminating the headache.

Acute Treatment of Migraine: The recommended dose of Rimegepant is 75 mg taken orally, as needed. The maximum dose in a 24-hour period is 75 mg. The safety of using more than 18 doses in a 30-day period has not been established.

Preventive Treatment of Episodic Migraine: The recommended dosage of Rimegepant is 75 mg taken orally every alternate day.

CYP3A4 Inhibitors: Concomitant administration of Apremig ODT with strong inhibitors of CYP3A4 results in a significant increase in Apremig ODT exposure. Avoid concomitant administration of Apremig ODT with strong inhibitors of CYP3A4. Concomitant administration of Apremig ODT with moderate inhibitors of CYP3A4 may result in increased exposure of Apremig ODT. Avoid another dose of Apremig ODT within 48 hours when it is concomitantly administered with moderate inhibitors of CYP3A4.
 
CYP3A Inducers: Concomitant administration of Apremig ODT with strong or moderate inducers of CYP3A can result in a significant reduction in Apremig ODT exposure, which may lead to loss of efficacy of Apremig ODT. Avoid concomitant administration of Apremig ODT with strong or moderate inducers of CYP3A.
 
P-gp Inhibitors: Concomitant administration of Apremig ODT with potent inhibitors of P-gp (e.g., amiodarone, cyclosporine, lapatinib, quinidine, ranolazine) may result in increased exposure of Apremig ODT. Avoid another dose of Apremig ODT within 48 hours when it is concomitantly administered with potent inhibitors of P-gp.

Rimegepant is contraindicated in patients with a history of hypersensitivity reaction to rimegepant, Sylvia ODT, or any of its components.

Allergic reactions, including trouble breathing and rash, can happen after you taking Apremig ODT. The most common side effects of Apremig ODT are: nausea, stomach pain & indigestion.

There are no adequate data on the developmental risk associated with the use of Rimegepant in pregnant women. There are no data on the presence of rimegepant or its metabolites in human milk, the effects of rimegepant on the breastfed infant, or the effects of rimegepant on milk production.

Hypersensitivity reactions, including dyspnea and rash, have occurred with Apremig ODT in clinical studies. Hypersensitivity reactions can occur days after administration, and delayed serious hypersensitivity has occurred. If a hypersensitivity reaction occurs, discontinue Apremig ODT and initiate appropriate therapy.

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
 
Geriatric Use: In pharmacokinetic studies, no clinically significant pharmacokinetic differences were observed between elderly and younger subjects. Clinical studies of Apremig ODT did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients.
 
Hepatic Impairment: No dosage adjustment of Apremig ODT is required in patients with mild (Child-Pugh A) or moderate (Child-Pugh B) hepatic impairment. Plasma concentrations of Apremig ODT were significantly higher in subjects with severe (Child-Pugh C) hepatic impairment. Avoid use of Apremig ODT in patients with severe hepatic impairment
 
Renal Impairment: No dosage adjustment of Apremig ODT is required in patients with mild, moderate, or severe renal impairment. Apremig ODT has not been studied in patients with end-stage renal disease and in patients on dialysis. Avoid use of Apremig ODT in patients with end-stage renal disease (CrCl<15 mL/min).

There is limited clinical experience with Apremig ODT overdosage. Treatment of an overdose of Apremig ODT should consist of general supportive measures including monitoring of vital signs and observation of the clinical status of the patient. No specific antidote for the treatment of Apremig ODT overdose is available. Apremig ODT is unlikely to be significantly removed by dialysis because of high serum protein binding.

Keep below 25°C temperature, away from light & moisture. Keep out of the reach of children.