Pizotifen (United States: Not available): Drug information

(For additional information see "Pizotifen (United States: Not available): Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)

Brand Names: Canada

Sandomigran DS;
Sandomigran [DSC]

Pharmacologic Category

Serotonin and Histamine Antagonist

Dosing: Adult

Migraine, prevention

Migraine, prevention (alternative agent):

Note: An adequate trial for assessment of effect is considered to be at least 2 to 3 months at a therapeutic dose (EHF [Steiner 2019]).

Oral: Initial: 0.5 mg at bedtime; may increase daily dose in 0.5 mg/day increments every week based on response and tolerability to 1.5 mg/day administered as a single dose at bedtime or in 3 divided doses; average maintenance dose: 1.5 mg/day. Maximum single dose: 3 mg/dose; maximum daily dose: 6 mg/day (CHS [Pringsheim 2012]; manufacturer's labeling).

Discontinuation of therapy: Avoid abrupt discontinuation to minimize withdrawal symptoms (eg, rebound headache, depression, nausea, tremor, anxiety, malaise, dizziness, sleep disorder, loss of consciousness, anorexia, rapid weight loss). The manufacturer recommends a gradual dose reduction over 2 weeks.

Missed dose: Patients taking ≥2 times daily: Administer the missed dose, as soon as possible. If there is <4 hours before the next scheduled dose, then skip the missed dose and resume regular dosing schedule. Do not double dose or administer more than maximum daily dose.

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

There are no dosage adjustments provided in the manufacturer’s labeling; however, dosage adjustments may be necessary. Use with caution.

Dosing: Hepatic Impairment: Adult

Hepatic impairment prior to treatment initiation:

There are no dosage adjustments provided in the manufacturer’s labeling; however, dosage adjustments may be necessary. Use with caution.

Hepatotoxicity during treatment:

Discontinue use; do not resume therapy until etiology of hepatic dysfunction is identified.

Dosing: Older Adult

Use with caution. Refer to adult dosing.

Dosing: Pediatric

Migraine, prophylaxis

Migraine, prophylaxis: Children ≥12 years and Adolescents: Oral: Initial: 0.5 mg at bedtime; may increase dose gradually up to maximum of 1 mg at bedtime or a maximum of 1.5 mg/day.

Note: Therapeutic response may require several weeks of therapy. Drug holidays are recommended periodically to assess the need for ongoing therapy. Do not discontinue abruptly (reduce gradually over 2-week period).

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: Pediatric

There are no dosage adjustments provided in the manufacturer’s labeling; however, dosage adjustments may be necessary. Use with caution.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer’s labeling; however, dosage adjustments may be necessary. Use with caution.

Adverse Reactions

The following adverse drug reactions are derived from product labeling unless otherwise specified.

Postmarketing:

Dermatologic: Skin rash, urticaria

Endocrine & metabolic: Amenorrhea, weight gain

Gastrointestinal: Constipation, increased appetite, nausea, xerostomia

Genitourinary: Breast hypertrophy, mastalgia, nonpuerperal lactation

Hepatic: Fulminant hepatitis, hepatic injury, hepatitis (can be severe), increased liver enzymes, jaundice

Hypersensitivity: Facial edema, hypersensitivity reaction

Nervous system: Anxiety, central nervous system stimulation (including agitation and aggressive behavior), depression, dizziness, drowsiness, fatigue, hallucination, insomnia, paresthesia, sedated state, seizure (including exacerbation of epilepsy), sleep disorder, withdrawal syndrome (following abrupt cessation of therapy)

Neuromuscular & skeletal: Arthralgia, muscle cramps, myalgia

Ophthalmic: Diplopia, increased intraocular pressure, mydriasis

Miscellaneous: Drug tolerance (prolonged use)

Contraindications

Hypersensitivity to pizotifen or any component of the formulation; concomitant use with or within 14 days following monoamine oxidase inhibitor therapy; gastric outlet obstruction (pyloroduodenal obstruction, stenosing pyloric ulcer); use in children <12 years of age.

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

Warnings/Precautions

Concerns related to adverse effects:

• Anticholinergic effects: Although anticholinergic effects (constipation, xerostomia, blurred vision, urinary retention) are limited, use with caution in patients with decreased gastrointestinal motility, myasthenia gravis, paralytic ileus, urinary retention, BPH, xerostomia, narrow-angle glaucoma, or other vision problems.

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Gradual titration of dose may help minimize sedative effects (eg, drowsiness).

• Hepatotoxicity: Hepatotoxic effects may occur with prolonged used; monitor liver function during therapy.

• Visual disturbances: Use has been associated with increased intraocular pressure, diplopia, and pupil dilation; limited number of patients experienced lens opacities but effect was not considered drug-related. Instruct patients to report visual disturbances during therapy.

• Weight gain/loss: Increased appetite and weight gain are common adverse effects; patients may experience rapid weight loss upon discontinuation. Use with caution in obese or other patients who may be vulnerable to these effects.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with cardiovascular disease.

• Diabetes: Use with caution in patients with diabetes mellitus.

• Epilepsy: Use with caution in patients with epilepsy; seizures have been reported very rarely with use.

• Hepatic impairment: Use with caution in patients with hepatic impairment. Dose adjustment may be necessary.

• Renal impairment: Use with caution in patients with renal impairment. Dose adjustment may be necessary.

Dosage forms specific issues:

• Lactose: May contain lactose; avoid use in patients with galactose or fructose intolerance, lactase deficiency, sucrose-isomaltase insufficiency, or glucose-galactose malabsorption.

Other warnings/precautions:

• Abrupt discontinuation: Avoid abrupt discontinuation which may cause acute withdrawal reactions (eg, depression, tremor, nausea, malaise, sleep disorder, dizziness, anxiety, loss of consciousness, anorexia and rapid weight loss); taper dosage over 2 weeks prior to discontinuation.

• Appropriate use: Not for use in acute treatment of migraine attacks or of tension headaches. Not considered first-line agent for migraine prophylaxis but may be considered when other therapies have failed (CHS [Pringsheim 2012]).

• Tolerance: May develop in some patients; effect may be overcome by dose increases (not to exceed maximum dosage). Consider drug-free period after several months of treatment.

Product Availability

Not available in the US

Generic Equivalent Available: US

Yes

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral:

Sandomigran: 0.5 mg [DSC] [contains fd&c yellow #5 (tartrazine)]

Sandomigran DS: 1 mg [contains fd&c yellow #5 (tartrazine)]

Administration: Adult

Oral: Administer daily dose as a single dose at bedtime or in divided doses; doses >3 mg should be administered in divided doses.

Administration: Pediatric

Oral: Administer daily dose as a single dose at bedtime or in divided doses

Children ≥12 years and Adolescents: Doses >1 mg should be administered in divided doses

Use: Labeled Indications

Note: Not available in the US.

Migraine, prevention: Prophylactic management of migraine.

Metabolism/Transport Effects

None known.

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.

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Amezinium: Antihistamines may enhance the stimulatory effect of Amezinium. Risk C: Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy

Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification

Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Betahistine may diminish the therapeutic effect of Antihistamines. Risk C: Monitor therapy

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider therapy modification

Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider therapy modification

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy

Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider therapy modification

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

Chlorprothixene: Anticholinergic Agents may enhance the anticholinergic effect of Chlorprothixene. Risk C: Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination

CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider therapy modification

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

Daridorexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider therapy modification

Difelikefalin: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Doxylamine: CNS Depressants may enhance the CNS depressant effect of Doxylamine. Risk C: Monitor therapy

DroPERidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination

Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination

Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Guanethidine: Pizotifen may diminish the therapeutic effect of Guanethidine. Risk C: Monitor therapy

Hyaluronidase: Antihistamines may diminish the therapeutic effect of Hyaluronidase. Risk C: Monitor therapy

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider therapy modification

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy

Ixabepilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kava Kava: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider therapy modification

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination

Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider therapy modification

Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy

Monoamine Oxidase Inhibitors: May enhance the anticholinergic effect of Pizotifen. Risk X: Avoid combination

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy

Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Oxybate Salt Products: CNS Depressants may enhance the CNS depressant effect of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interrupt oxybate salt treatment during short-term opioid use Risk D: Consider therapy modification

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy

Pitolisant: Antihistamines may diminish the therapeutic effect of Pitolisant. Risk X: Avoid combination

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid combination

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination

Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy

Reserpine: Pizotifen may diminish the antihypertensive effect of Reserpine. Risk C: Monitor therapy

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination

Rivastigmine: Anticholinergic Agents may diminish the therapeutic effect of Rivastigmine. Rivastigmine may diminish the therapeutic effect of Anticholinergic Agents. Management: Use of rivastigmine with an anticholinergic agent is not recommended unless clinically necessary. If the combination is necessary, monitor for reduced anticholinergic effects. Risk D: Consider therapy modification

Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider therapy modification

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider therapy modification

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider therapy modification

Zuranolone: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider therapy modification

Reproductive Considerations

In general, preventive treatment for migraine in patients trying to become pregnant should be avoided. Options for patients planning a pregnancy should be considered as part of a shared decision-making process. Nonpharmacologic interventions should be considered initially. When needed, preventive treatment should be individualized considering the available safety data and needs of the patient should pregnancy occur. A gradual discontinuation of preventive medications is generally preferred when the decision is made to stop treatment prior to conception (ACOG 2022; AHS [Ailani 2021]).

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies.

In general, preventive treatment for migraine should be avoided during pregnancy. Options for pregnant patients should be considered as part of a shared decision-making process. Nonpharmacologic interventions should be considered initially. When needed, preventive treatment should be individualized considering the available safety data, potential for adverse maternal and fetal events, and needs of the patient (ACOG 2022; AHS [Ailani 2021]).

If preventive therapy is needed, agents other than pizotifen are preferred (CHS [Pringsheim 2012]).

Breastfeeding Considerations

It is not known if pizotifen is present in breast milk (Davanzo 2014).

According to the manufacturer, pizotifen is unlikely to affect a breastfeeding infant; however, use is not recommended in breastfeeding patients. In general, preventive treatment for migraine in breastfeeding patients should be avoided. When needed, therapy should be individualized considering the available safety data and needs of the patient (AHS [Ailani 2021]). If preventive therapy is needed, agents other than pizotifen are preferred (CHS [Pringsheim 2012]).

Monitoring Parameters

Hepatic function tests (prolonged use); renal function tests; weight gain; BP; visual disturbance.

Mechanism of Action

Pizotifen is a strong serotonin and tryptamine antagonist with weak antihistamine, anticholinergic and antikinin effects; also has appetite-stimulating and sedative properties. The mechanism of action in migraine prophylaxis has not been fully elucidated; may alter pain thresholds by inhibiting the permeability increasing effect of serotonin and histamine to control movement of plasmakinin across cranial vessel membranes. Inhibits serotonin reuptake by platelets, affecting tonicity and reducing passive distension of extracranial arteries.

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: May require several weeks of therapy

Distribution: V_d: Parent drug: 833 L; N-glucuronide metabolite: 70 L

Protein binding: >90%

Metabolism: Hepatic (mainly by glucuronidation)

Bioavailability: 78%

Half-life elimination: ~23 hours (parent drug and N-glucuronide metabolite)

Time to peak: 5 hours

Excretion: Feces (~33% of dose); urine (55% as metabolites, <1% as unchanged drug)

Brand Names: International

International Brand Names by Country

For country code abbreviations (show table)

(AE) United Arab Emirates: Migranil | Mosegor;
(AR) Argentina: Sandomigran;
(AU) Australia: Sandomigran;
(BD) Bangladesh: Antigrain | Avidro | Dmigrain | Migrafen | Migranex | Migranil | Pifen | Pitofen | Pizo-A | Pizofen | Pizotin | Zeromig | Zofen | Zonil;
(BE) Belgium: Sandomigran;
(BR) Brazil: Sandomigran;
(CH) Switzerland: Mosegor | Sandomigran;
(CN) China: Pizotifen | Pizotyline;
(CO) Colombia: Mosegor | Sandomigran;
(CZ) Czech Republic: Sandomigran;
(DE) Germany: Sandomigran;
(DO) Dominican Republic: Mosegor | Sandomigran;
(EC) Ecuador: Mosegor;
(EE) Estonia: Sandomigran;
(EG) Egypt: Mosegor;
(ES) Spain: Mosegor | Sandomigran;
(FI) Finland: Sandomigrin;
(FR) France: Sanmigran;
(GB) United Kingdom: Pizotifen | Pizotifen cox | Pizotifen kent | Sanomigran;
(HK) Hong Kong: Sandomigran;
(HU) Hungary: Sandomigran;
(ID) Indonesia: Litec | Lysagor;
(IE) Ireland: Pizotifen | Sanomigran;
(IL) Israel: Sandomigran;
(IT) Italy: Sandomigran;
(JO) Jordan: Pizofen | Sandomigran;
(KR) Korea, Republic of: Litec;
(LB) Lebanon: Mosegor;
(LT) Lithuania: Sandomigran;
(LU) Luxembourg: Mosegor | Sandomigran;
(LV) Latvia: Sandomigran;
(MA) Morocco: Sanmigran;
(MX) Mexico: Sandomigran;
(MY) Malaysia: Acugrain | Pizogran | Sandomigran;
(NG) Nigeria: Mosegor;
(NL) Netherlands: Sandomigran;
(NZ) New Zealand: Sandomigran;
(PH) Philippines: Litec;
(PK) Pakistan: Cestonil | Mosegor | Pifin | Pizofen | Zofin;
(PL) Poland: Polomigran | Sandomigran;
(PT) Portugal: Mosegor | Sandomigrane;
(QA) Qatar: Mosegor;
(SA) Saudi Arabia: Mosegor;
(SE) Sweden: Sandomigrin;
(SK) Slovakia: Sandomigran;
(TH) Thailand: Anorsia | Migrin | Migsin | Mizekor | Mosegor | Moselar | Mozifen | Pizo | Pizomed | Pizotifen | Sandomigran | Sosegor | Suzi | Zofen | Zuzi;
(TN) Tunisia: Pizofen | Sanmigran;
(TR) Turkey: Mosegor | Sandomigran;
(UA) Ukraine: Profimig;
(UY) Uruguay: Sandomigran;
(VE) Venezuela, Bolivarian Republic of: Sandomiran;
(ZA) South Africa: Sandomigran;
(ZW) Zimbabwe: Sandomigran

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]
American College of Obstetricians and Gynecologists (ACOG). 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]
Davanzo R, Bua J, Paloni G, Facchina G. Breastfeeding and migraine drugs. Eur J Clin Pharmacol. 2014;70(11):1313-1324. doi:10.1007/s00228-014-1748-0 [PubMed 25217187]
Elouni B, Ben Salem C, Zamy M, et al, “Fulminant Hepatitis Possibly Related to Pizotifen Therapy,” Ann Pharmacother, 2010, 44(7-8):1348-9. [PubMed 20571104]
Pringsheim T, Davenport W, Mackie G, et al. Canadian Headache Society guideline for migraine prophylaxis. Can J Neurol Sci. 2012;39(2)(suppl 2):1-59. [PubMed 22683887]
Sandomigran and Sandomigran DS (pizotifen) [product monograph]. Montreal, Quebec, Canada: Paladin Labs, Inc; October 2012.
Sandomigran DS (pizotifen) [product monograph]. Saint-Laurent, Quebec, Canada: Paladin Labs Inc; August 2023.
Steiner TJ, Jensen R, Katsarava Z, et al. Aids to management of headache disorders in primary care (2nd edition): on behalf of the European Headache Federation and Lifting The Burden: the Global Campaign Against Headache. J Headache Pain. 2019;20(1):57. doi:10.1186/s10194-018-0899-2 [PubMed 31113373]

Topic 10091 Version 222.0

خرید پکیج

Pizotifen (United States: Not available): Drug information