ﺑﺎﺯﮔﺸﺖ ﺑﻪ ﺻﻔﺤﻪ ﻗﺒﻠﯽ
خرید پکیج
تعداد آیتم قابل مشاهده باقیمانده : 3 مورد
نسخه الکترونیک
medimedia.ir

Zavegepant: Drug information

Zavegepant: Drug information
(For additional information see "Zavegepant: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Zavzpret
Pharmacologic Category
  • Antimigraine Agent;
  • Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist
Dosing: Adult
Migraine, moderate to severe, acute treatment

Migraine, moderate to severe, acute treatment (alternative agent):

Note: Consider use if triptans are contraindicated (eg, cardiovascular risk factors), ineffective, or poorly tolerated. Administration early in the course of a migraine attack, at the first sign of pain, may improve response to treatment (Ref).

Intranasal: One spray (10 mg/spray) in 1 nostril as a single dose. Maximum: One spray (10 mg) per 24 hours (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

CrCl ≥30 mL/minute: No dosage adjustment necessary.

CrCl <30 mL/minute: Avoid use.

Dosing: Hepatic Impairment: Adult

Mild to moderate impairment (Child-Pugh class A, B): No dosage adjustment necessary.

Severe impairment (Child-Pugh class C): Avoid use.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults.

>10%: Gastrointestinal: Taste disorder (18%)

1% to 10%:

Gastrointestinal: Nausea (4%), vomiting (2%)

Respiratory: Nasal discomfort (3%)

<1%: Hypersensitivity: Hypersensitivity reaction (including facial swelling)

Contraindications

Hypersensitivity to zavegepant or any component of the formulation.

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity reactions: Hypersensitivity reactions, including facial swelling and urticaria, may occur. Discontinue use and institute appropriate therapy if a hypersensitivity reaction occurs.

Disease-related concerns:

• Hepatic impairment: Use is not recommended in patients with severe hepatic impairment.

• Renal impairment: Use is not recommended in patients with severe renal impairment (CrCl <30 mL/minute).

Other warnings/precautions:

• Appropriate use: The safety of treating more than 8 migraines in a 30-day period has not been established.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Nasal:

Zavzpret: 10 mg/actuation (1 ea, 6 ea)

Generic Equivalent Available: US

No

Pricing: US

Solution (Zavzpret Nasal)

10 mg/ACT (per each): $220.00

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Intranasal: For intranasal administration only. Avoid concomitant administration with intranasal decongestants due to decreased zavegepant absorption; if intranasal decongestants must be used, administer ≥1 hour after zavegepant administration. Keep device in sealed blister pack until ready to use; each device is single use and contains only 1 dose. Do not test spray, prime, or press the plunger before use. While sitting or standing, gently blow nose to clear nostrils. Hold device upright with thumb on bottom of the plunger and 2 fingers on either side of the nozzle. With other hand, close 1 nostril gently. While keeping head level and upright, and mouth closed, insert nozzle into open nostril as far as comfortable. Instruct patient to slowly breathe in through nose and press plunger firmly with thumb to release spray; retain nozzle in nose during dose administration; do not remove nozzle while pressing plunger. Do not tilt head or lay down while delivering dose. Remove nozzle from nostril; keep head level for 10 to 20 seconds and gently breathe in through nose and out through mouth. If nose starts dripping, gently sniff to avoid losing any of the dose.

Use: Labeled Indications

Migraine, moderate to severe, acute treatment: Acute treatment of migraine with or without aura in adults (AHS [Ailani 2021]; Lipton 2023; manufacturer's labeling).

Limitations of use: Not indicated for the preventive treatment of migraine.

Metabolism/Transport Effects

Substrate of CYP2D6 (minor), CYP3A4 (minor), OATP1B1/1B3 (SLCO1B1/1B3), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Asciminib: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy

Decongestants (Nasally Administered): May decrease the serum concentration of Zavegepant. Management: Avoid the concurrent administration of intranasal decongestants with zavegepant. If combined use is unavoidable, intranasal decongestants should be administered at least 1 hour after zavegepant administration. Risk D: Consider therapy modification

Leniolisib: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid combination

OATP1B1/1B3 (SLCO1B1/1B3) Inducers: May decrease the serum concentration of Zavegepant. Risk X: Avoid combination

OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors: May increase the serum concentration of Zavegepant. Risk X: Avoid combination

Pretomanid: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy

Trofinetide: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Management: Avoid concurrent use with OATP1B1/1B3 substrates for which small changes in exposure may be associated with serious toxicities. Monitor for evidence of an altered response to any OATP1B1/1B3 substrate if used together with trofinetide. Risk D: Consider therapy modification

Voclosporin: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies following SUBQ administration.

Zavegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist. Based on animal data, CGRP may help regulate placental blood flow, uterine relaxation, and maintain BP; CGRP antagonists could potentially increase the risk of gestational hypertension and preeclampsia (Dodick 2019). The risk of hypertensive disorders, including preeclampsia and eclampsia, are also increased in pregnant patients with migraine (ACOG 2022; Dodick 2019).

Treatment of migraine during pregnancy should be individualized considering the available safety data, the potential for adverse maternal and fetal events, and needs of the patient (AHS [Ailani 2021]). CGRP receptor antagonists are not currently recommended for the treatment of acute migraine in pregnant patients due to lack of data (ACOG 2022).

Breastfeeding Considerations

It is not known if zavegepant is present in breast milk.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Treatment of migraine in lactating patients should be individualized considering the available safety data and needs of the patient (AHS [Ailani 2021]). Calcitonin gene-related peptide receptor antagonists are not currently recommended for the treatment of acute migraine in lactating patients due to lack of data (ACOG 2022).

Mechanism of Action

Zavegepant is a calcitonin gene-related peptide receptor antagonist.

Pharmacokinetics (Adult Data Unless Noted)

Onset: Pain relief: May occur as early as 15 minutes post administration (Lipton 2023).

Absorption: Rapid (Lipton 2023).

Distribution: Vd: ~1,774 L.

Protein binding: ~90%.

Metabolism: Primarily via CYP3A4 and to a lesser extent via CYP2D6.

Bioavailability: ~5%.

Half-life elimination: 6.55 hours.

Time to peak: ~30 minutes.

Excretion: Feces: ~80%; urine: ~11%.

  1. Ailani J, Burch RC, Robbins MS; Board of Directors of the American Headache Society. The American Headache Society consensus statement: update on integrating new migraine treatments into clinical practice. Headache. 2021;61(7):1021-1039. doi:10.1111/head.14153 [PubMed 34160823]
  2. American College of Obstetricians and Gynecologists (ACOG). ACOG Committee on Clinical Practice Guidelines–Obstetrics. Headaches in pregnancy and postpartum: ACOG clinical practice guideline no. 3. Obstet Gynecol. 2022;139(5):944-972. doi:10.1097/AOG.0000000000004766 [PubMed 35576364]
  3. Dodick DW. CGRP ligand and receptor monoclonal antibodies for migraine prevention: evidence review and clinical implications. Cephalalgia. 2019;39(3):445-458. doi:10.1177/0333102418821662 [PubMed 30661365]
  4. Lipton RB, Croop R, Stock DA, et al. Safety, tolerability, and efficacy of zavegepant 10 mg nasal spray for the acute treatment of migraine in the USA: a phase 3, double-blind, randomised, placebo-controlled multicentre trial. Lancet Neurol. 2023;22(3):209-217. doi:10.1016/S1474-4422(22)00517-8 [PubMed 36804093]
  5. Refer to manufacturer's labeling.
  6. Zavzpret (zavegepant) [prescribing information]. New York, NY: Pfizer Labs; March 2023.
Topic 140988 Version 30.0

آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟