Pizotifen (Mosegor, Sandomigran) belongs to the drug class called antamines. It is a potent inhibitor of serotonin and tryptamine.
Pizotifen Uses:
- Note: Not available in the US
-
Migraine prophylaxis:
- Prophylactic management of migraine.
Pizotifen dose in Adults
Pizotifen dose in the prophylaxis of Migraine:
- Oral: Initial:0.5 mg before bed; progressively raise the dose to 1.5 mg daily, either in one dose at night or in three smaller doses; average maintenance dose: 1.5 mg daily; typical dosage range: 1 to 6 mg daily (maximum dose: 6 mg/day).
Note:
- Several weeks of therapy may be necessary to see a therapeutic response.
- Periodically, drug holidays are advised to determine whether continued therapy is necessary.
- Avoid stopping abruptly.
Pizotifen dose in Children
Pizotifen (Sandomigran) dose in the prophylaxis of Migraine:
-
Children ≥12 years and Adolescents:
- Oral: Initial dose: 0.5 mg before bed. The dose may be gradually raised up to a maximum of 1 mg before night or a maximum of 1.5 mg per day.
Note:
- Several weeks of therapy may be necessary to see a therapeutic response.
- Periodically, drug holidays are advised to determine whether continued therapy is necessary.
- Avoid stopping abruptly (reduce gradually over the 2-week period).
Pizotifen Pregnancy Risk Category: B1
- In animal reproduction studies, adverse events were not reported.
- Pregnancy should be avoided if possible.
- Other agents are preferable if therapy is required.
Use of Pizotifen while breastfeeding
- Nursing infants are unlikely to be affected by the pizotifen concentration in breast milk.
- However, the drug manufacturer doesn't recommend that nursing mothers use the drug.
- Nursing women should avoid prophylactic medication for migraines if possible.
- Other agents are preferable if therapy is required.
Pizotifen Dose in Kidney Disease:
- There are no dosage adjustments provided in the drug manufacturer’s labeling; however, dosage adjustments may be necessary.
- Use with caution.
Pizotifen dose in Liver Disease:
- There are no dosage adjustments provided in the drug manufacturer’s labeling; however, dosage adjustments may be necessary.
- Use with caution.
Common Side Effects of Pizotifen (Mosegor):
-
Endocrine & metabolic:
- Weight gain
-
Gastrointestinal:
- Increased appetite
Less Common Side Effects of Pizotifen (Mosegor):
-
Central nervous system:
- Dizziness
- Drowsiness (including fatigue)
-
Gastrointestinal:
- Nausea
- Xerostomia
Contraindications to Pizotifen:
- Hypersensitivity or allergy
- Concurrent use of MAO inhibitors
- Gastric outlet obstruction (pyloroduodenal obstruction, or stenosing piloric ulcer)
- Use in children under 12 years old
Warnings and precautions
-
Anticholinergic effects
- While anticholinergic effects such as constipation, xerostomia and blurred vision are not common, it is important to use caution in patients with myasthenia gravis or paralytic ileus.
- Ophthalmic screening is highly recommended.
-
Depression in the CNS:
- CNS depression can lead to impairment of mental or physical abilities. Patients should be cautious about driving or operating machinery that requires mental alertness.
- Gradual titration may be helpful in reducing sedative effects (eg drowsiness).
-
Hepatotoxicity
- Long-term use may cause liver toxic effects.
- During therapy, it is recommended to have a periodic assessment of the liver function.
- Stop using hepatic dysfunction signs and symptoms. Do not resume therapy until you have identified the cause.
-
Visual disturbances
- It has been linked to increased intraocular pressure, diplopia and pupil dilation.
- A small number of patients experienced lenses opacities, but this effect was not thought to be drug-related.
- Encourage patients to report any visual impairments during therapy.
-
Weight loss/gain
- Patients may notice an increase in appetite or weight gain.
- These effects may be more severe in obese patients or patients who are already at risk.
-
Cardiovascular disease
- Patients with heart disease should be cautious.
-
Diabetes:
- Patients with diabetes mellitus should be cautious.
-
Epilepsy:
- Patients with epilepsy should be cautious; seizures are very rare with this medication.
-
Hepatic impairment
- Patients with hepatic impairment should be cautious.
- Sometimes, dose adjustment is necessary.
-
Renal impairment
- Patients with impaired renal function should be cautious.
- Sometimes, dose adjustment is necessary.
Pizotifen (United States: Not available): Drug Interaction
|
Acetylcholinesterase Inhibitors |
May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. |
|
Alcohol (Ethyl) |
Alcohol's CNS depressing effect may be amplified by CNS depressants (Ethyl). |
|
Alizapride |
CNS depressants may have an enhanced CNS depressant impact. |
|
Amantadine |
May strengthen an anticholinergic agent's anticholinergic action. |
|
Amezinium |
Antihistamines may intensify Amezinium's stimulant effects. |
|
Amphetamines |
May lessen antihistamines' sedative effects. |
|
Anticholinergic Agents |
Other anticholinergic agents' negative or hazardous effects might be amplified. |
|
Betahistine |
Betahistine's therapeutic impact may be reduced by antihistamines. |
|
Botulinum Toxin-Containing Products |
May enhance the anticholinergic effect of Anticholinergic Agents. |
|
Brexanolone |
CNS Depressants may enhance the CNS depressant effect of Brexanolone. |
|
Brimonidine (Topical) |
May enhance the CNS depressant effect of CNS Depressants. |
|
Bromopride |
May enhance the CNS depressant effect of CNS Depressants. |
|
Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
|
Cannabis |
May enhance the CNS depressant effect of CNS Depressants. |
|
Chloral Betaine |
May enhance the adverse/toxic effect of Anticholinergic Agents. |
|
Chlorphenesin Carbamate |
May enhance the adverse/toxic effect of CNS Depressants. |
|
CNS Depressants |
May enhance the adverse/toxic effect of other CNS Depressants. |
|
Dimethindene (Topical) |
May enhance the CNS depressant effect of CNS Depressants. |
|
Doxylamine |
May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. |
|
Dronabinol |
May enhance the CNS depressant effect of CNS Depressants. |
|
Esketamine |
May enhance the CNS depressant effect of CNS Depressants. |
|
Gastrointestinal Agents (Prokinetic) |
Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). |
|
Glucagon |
Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. |
|
Guanethidine |
Pizotifen may diminish the therapeutic effect of Guanethidine. |
|
HydrOXYzine |
May enhance the CNS depressant effect of CNS Depressants. |
|
Itopride |
Anticholinergic Agents may diminish the therapeutic effect of Itopride. |
|
Kava Kava |
May enhance the adverse/toxic effect of CNS Depressants. |
|
Lofexidine |
May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
|
Magnesium Sulfate |
May enhance the CNS depressant effect of CNS Depressants. |
|
MetyroSINE |
CNS Depressants may enhance the sedative effect of MetyroSINE. |
|
Mianserin |
May enhance the anticholinergic effect of Anticholinergic Agents. |
|
Minocycline |
May enhance the CNS depressant effect of CNS Depressants. |
|
Mirabegron |
Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. |
|
Mirtazapine |
CNS Depressants may enhance the CNS depressant effect of Mirtazapine. |
|
Nabilone |
May enhance the CNS depressant effect of CNS Depressants. |
|
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. |
|
Piribedil |
CNS Depressants may enhance the CNS depressant effect of Piribedil. |
|
Pramipexole |
CNS Depressants may enhance the sedative effect of Pramipexole. |
|
Ramosetron |
Anticholinergic Agents may enhance the constipating effect of Ramosetron. |
|
Reserpine |
Pizotifen may diminish the antihypertensive effect of Reserpine. |
|
ROPINIRole |
CNS Depressants may enhance the sedative effect of ROPINIRole. |
|
Rotigotine |
CNS Depressants may enhance the sedative effect of Rotigotine. |
|
Rufinamide |
May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. |
|
Selective Serotonin Reuptake Inhibitors |
CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. |
|
Tetrahydrocannabinol |
May enhance the CNS depressant effect of CNS Depressants. |
|
Tetrahydrocannabinol and Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
|
Thiazide and Thiazide-Like Diuretics |
Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. |
|
Topiramate |
Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. |
|
Trimeprazine |
May enhance the CNS depressant effect of CNS Depressants. |
|
Risk Factor D (Consider therapy modification) |
|
|
Benzylpenicilloyl Polylysine |
Antihistamines may reduce Benzylpenicilloyl Polylysine's ability to diagnose. Management: Delay testing until systemic antihistaminic effects have subsided and discontinue systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing. To determine whether permanent antihistaminic effects exist, a histamine skin test may be utilised. |
|
Blonanserin |
CNS Depressants may enhance the CNS depressant effect of Blonanserin. |
|
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. |
|
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. |
|
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. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
|
Flunitrazepam |
CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. |
|
Hyaluronidase |
Antihistamines may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving antihistamines (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required. |
|
HYDROcodone |
CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone 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. |
|
Methotrimeprazine |
CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. |
|
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. |
|
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. |
|
Perampanel |
May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. |
|
Pramlintide |
May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. |
|
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. |
|
Sodium Oxybate |
May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. |
|
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. |
|
Tapentadol |
May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol 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. |
|
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 Factor X (Avoid combination) |
|
|
Aclidinium |
May enhance the anticholinergic effect of Anticholinergic Agents. |
|
Azelastine (Nasal) |
CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). |
|
Bromperidol |
May enhance the CNS depressant effect of CNS Depressants. |
|
Cimetropium |
Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. |
|
Eluxadoline |
Anticholinergic Agents may enhance the constipating effect of Eluxadoline. |
|
Glycopyrrolate (Oral Inhalation) |
Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). |
|
Glycopyrronium (Topical) |
May enhance the anticholinergic effect of Anticholinergic Agents. |
|
Ipratropium (Oral Inhalation) |
May enhance the anticholinergic effect of Anticholinergic Agents. |
|
Levosulpiride |
Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. |
|
Monoamine Oxidase Inhibitors |
May enhance the anticholinergic effect of Pizotifen. |
|
Orphenadrine |
CNS Depressants may enhance the CNS depressant effect of Orphenadrine. |
|
Oxatomide |
May enhance the anticholinergic effect of Anticholinergic Agents. |
|
Oxomemazine |
May enhance the CNS depressant effect of CNS Depressants. |
|
Paraldehyde |
CNS Depressants may enhance the CNS depressant effect of Paraldehyde. |
|
Pitolisant |
Antihistamines may diminish the therapeutic effect of Pitolisant. |
|
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. |
|
Potassium Citrate |
Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. |
|
Revefenacin |
Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. |
|
Thalidomide |
CNS Depressants may enhance the CNS depressant effect of Thalidomide. |
|
Tiotropium |
Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. |
|
Umeclidinium |
May enhance the anticholinergic effect of Anticholinergic Agents. |
Monitoring Parameters:
- Hepatic function tests (prolonged use);
- renal function tests,
- weight gain;
- blood pressure
How to administer Pizotifen (Mosegor)?
- Oral: Administer daily dose as a single dose at bedtime or in divided doses;
- Doses >3 mg should be administered in divided doses.
Mechanism of action of Pizotifen (Mosegor):
- Pizotifen, a strong tryptamine and serotonin antagonist, has weak antihistamine and anticholinergic effects.
- It has both appetite-stimulating as well as sedative properties.
- It is not clear what mechanism works in migraine prophylaxis.
- It can alter pain thresholds by decreasing the permeability-increasing effects of serotonin, histamine and to control the movement plasma kinin across the cranial vessel membranes.
- It inhibits serotonin reuptake from platelets, which can affect tonicity and reduce passive distension of extracranial arterial arteries.
The onset of action:
- May require several weeks of therapy
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 the dose);
- urine (55% as metabolites, <1% as unchanged drug)
International Brands of Pizotifen:
- Sandomigran
- Sandomigran DS
- Acugrain
- Anorsia
- Apizine
- Avidro
- Duotifen
- Lematite
- Litec
- Lysagor
- Migranex
- Mor-Vita
- Mosegor
- Mozifen-EF
- Pizofen
- Pizogran
- Pizomed
- Raiteck
- Sandmigrin
- Sandomigran
- Sandomigrin
- Zofen
- Zonil
Pizotifen Brand Names in Pakistan:
Pizotifen (Hydrogen Maleate) 0.5 mg Syrup |
|
| Mozgor | Jawa Pharmaceuticals(Pvt) Ltd. |
| Pizopro | Goodman Laboratories |
Pizotifen (Hydrogen Maleate) 0.5 mg/5ml Syrup |
|
| Alsigor | Alson Pharmaceuticals |
| Merigor | Miracle Pharmaceuticals(Pvt) Ltd |
Pizotifen (Hydrogen Maleate) 0.25 mg/5ml Syrup |
|
| Anarex | Imco Pharmaceuticals Laboratories |
| Aptigar | Evergreen Pharmaceuticals Pvt Limited |
| Cestonil | Raazee Theraputics (Pvt) Ltd. |
| Lowfen | Lowitt Pharmaceuticals (Pvt) Ltd |
| Mosegor | Novartis Pharma (Pak) Ltd |
| Movigar | Olive Laboratories |
| Neosegor | Neo Medix |
| Pifin | Libra Pharmaceuticals (Pvt) Ltd |
| Pizo | English Pharmaceuticals Industries |
| Pizofen | Alina Combine Pharmaceuticals (Pvt) Ltd. |
| Pizogar | Alliance Pharmaceuticals (Pvt) Ltd. |
| Pizosel | Selmore Agencies |
| Pizosun | Hisun Pharmaceuticals |
| Zigor | Onyx Pharmaceutical |
Pizotifen (Hydrogen Maleate) 0.5 mg/10ml Syrup |
|
| Mosor | Fynk Pharmaceuticals |
| Pizolam | Paramount Pharmaceuticals |
Pizotifen (Hydrogen Maleate) 0.5 mg Tablets |
|
| Apitiz | Swiss Pharmaceuticals (Pvt) Ltd. |
| Cestonil | Raazee Theraputics (Pvt) Ltd. |
| Mosegor | Novartis Pharma (Pak) Ltd |
| Movigar | Olive Laboratories |
| Pifin | Libra Pharmaceuticals (Pvt) Ltd |
| Pizofen | Alina Combine Pharmaceuticals (Pvt) Ltd. |
