Qulipta (Tablets) Instructions for Use

Marketing Authorization Holder

AbbVie, LLC (Russia)

Manufactured By

Forest Laboratories Ireland, Ltd. (Ireland)

ATC Code

N02CD07 (Atogepant)

Active Substance

Atogepant (Rec.INN registered by WHO)

Dosage Forms

	Qulipta	Tablets 10 mg
		Tablets 60 mg

Dosage Form, Packaging, and Composition

Tablets

7 pcs. – blisters (4 pcs.) – cardboard packs (28 pcs.) – By prescription

Tablets

7 pcs. – blisters (4 pcs.) – cardboard packs (28 pcs.) – By prescription

Pharmacotherapeutic Group

Analgesics; antimigraine preparations; CGRP (calcitonin gene-related peptide) antagonists

Pharmacological Action

Atogepant is a low molecular weight selective antagonist of the calcitonin gene-related peptide (CGRP) receptor for oral administration, which blocks the binding of CGRP to the receptor and suppresses CGRP receptor function. CGRP is a neuropeptide associated with the pathophysiology of migraine. In the trigeminovascular system, CGRP modulates the transmission of nociceptive signals and inflammation, and also has a vasodilatory effect.

At a dose five times the maximum recommended daily dose, Atogepant does not prolong the QT interval to a clinically significant extent.

Pharmacokinetics

After oral administration, Atogepant is rapidly absorbed, with its plasma concentration exceeding 14 nmol/L (90% effective concentration (EC₉₀) in a model of capsaicin-induced skin vasodilation) on average after 0.5 h, and the median time to reach C_max ranges from 1 to 2 h. The binding of atogepant to plasma proteins was independent of concentration in the range from 0.1 to 10 µmol/L; the unbound fraction of atogepant in human plasma was about 4.7%. The mean apparent V_d of atogepant after oral administration is about 292 L.

Atogepant is primarily eliminated by metabolism, predominantly via CYP3A4. Unchanged Atogepant and its conjugated metabolite (glucuronide, M23) were the most common circulating compounds in human plasma.

The T_1/2 of atogepant is about 11 h. The mean total plasma clearance of atogepant after oral administration is about 19 L/h. After a single dose of 50 mg of ¹⁴C-atogepant in healthy men, 42% and 5% of the administered dose was excreted as unchanged atogepant in feces and urine, respectively.

Indications

Preventive treatment of migraine occurring at least 4 days per month in adults aged 18 years and older.

ICD codes

Dosage Regimen

Take orally once daily. The recommended dose for most patients is 60 mg.

For patients with severe renal impairment (CrCl 15-29 mL/min) or end-stage chronic kidney disease (CrCl <15 mL/min), use the 10 mg dose once daily.

If you are on intermittent hemodialysis, take the 10 mg dose after the dialysis procedure.

No dose adjustment is required for patients with mild or moderate hepatic impairment (Child-Pugh class A or B).

Avoid use in patients with severe hepatic impairment (Child-Pugh class C).

No dose adjustment is required for elderly patients.

Take the tablet with or without food. Swallow the tablet whole with water; do not split, crush, or chew.

If a dose is missed, take it as soon as you remember. If it is almost time for the next dose, skip the missed dose and resume the regular schedule. Do not take a double dose to make up for a forgotten one.

Adverse Reactions

Immune system disorders unknown – hypersensitivity reactions.

Metabolism and nutrition disorders common – decreased appetite.

Gastrointestinal disorders common – nausea, constipation.

General disorders and administration site conditions common – fatigue/somnolence.

Investigations common – weight decrease; uncommon – increased ALT and AST.

Contraindications

Hypersensitivity to atogepant, pregnancy, breastfeeding period, children and adolescents under 18 years of age.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

In patients with mild or moderate renal impairment, no dose adjustment of the drug is required.
In patients with severe renal impairment (CrCl 15-29 mL/min) and in patients with end-stage chronic kidney disease (CrCl < 15 mL/min), the recommended dose is 10 mg once daily. For patients with end-stage chronic kidney disease on intermittent hemodialysis, Atogepant should be taken after
The dialysis procedure.

Use in Renal Impairment

In patients with mild (Child-Pugh class A) or moderate (Child-Pugh class B) hepatic impairment, no dose adjustment is required.

Use should be avoided in patients with severe hepatic impairment (Child-Pugh class C).

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

No dose adjustment is required in elderly patients.

Special Precautions

Most serious hypersensitivity reactions developed within 24 hours of the first use of atogepant. However, some hypersensitivity reactions may occur several days after atogepant administration. Patients should be advised about symptoms associated with hypersensitivity reactions. In case of a hypersensitivity reaction, atogepant should be discontinued and appropriate therapy initiated.

Effect on ability to drive and operate machinery

Has no or negligible influence on the ability to drive and use machines. However, somnolence may occur in some cases. Patients should be cautioned about driving or using machinery until they are reasonably sure that Atogepant does not adversely affect these activities.

Drug Interactions

Concomitant administration of atogepant with itraconazole, a strong CYP3A4 inhibitor, resulted in a significant increase in the systemic exposure of atogepant in healthy volunteers. When used concomitantly with moderate or weak CYP3A4 inhibitors, no dose adjustment of atogepant is required.

Concomitant administration of atogepant with a single dose of rifampicin, an OATP inhibitor, resulted in a significant increase in the systemic exposure of atogepant in healthy volunteers.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.