Drug Action
Selegiline is a monoamine-oxidase-B inhibitor.
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Drug reference
Selegiline is a monoamine-oxidase-B inhibitor.
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Parkinson’s disease, used alone or as adjunct to co- Nervous system beneldopa or co-careldopa to reduce ’end of dose’ deterioration | Symptomatic parkinsonism ▶BY MOUTH USING IMMEDIATE-RELEASE MEDICINES ▶Adult: Initially 5 mg once daily for 2–4 weeks, then increased if tolerated to 10 mg daily, dose to be taken in the morning ▶BY MOUTH USING ORAL LYOPHILISATE ▶Adult: 1.25 mg once daily, dose to be taken before breakfast DOSE EQUIVALENCE AND CONVERSION ▶1.25-mg oral lyophilisate is equivalent to 10-mg tablet. ▶Patients receiving 10 mg conventional selegiline hydrochloride tablets can be switched to oral lyophilisates (Zelapar ®) 1.25 mg.
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Active duodenal ulceration. active gastric ulceration. avoid or use with great caution in postural hypotension (when used in combination with levodopa)
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Angina. arrhythmias. duodenal ulceration. gastric ulceration. history of hepatic dysfunction. patients predisposed to confusion and psychosis. psychosis. uncontrolled hypertension
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→Appendix 1: MAO-B inhibitors
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▶Common or very common Arrhythmias. arthralgia. back pain. confusion. constipation. depression. diarrhoea. dizziness. dry mouth. fall. fatigue. hallucination. headache. hyperhidrosis. hypertension. hypotension. movement disorders. muscle cramps. nasal congestion. nausea. oral disorders. sleep disorders. throat pain. tremor. vertigo ▶Uncommon Alopecia. angina pectoris. anxiety. appetite decreased. chest pain. dyspnoea. leucopenia. mood altered. myopathy. palpitations. peripheral oedema. pharyngitis. psychosis. skin eruption. thrombocytopenia. urinary disorders. vision blurred ▶Frequency not known Hypersexuality SIDE-EFFECTS, FURTHER INFORMATION Side-effects of levodopa may be increased—concurrent levodopa dosage can be reduced by 10–30% in steps of 10% every 3–4 days.
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Avoid—no information available.
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Avoid—no information available.
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Manufacturer advises caution in severe impairment.
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Use with caution in severe impairment.
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Oral lyophilisates should be placed on the tongue and allowed to dissolve. Advise patient not to drink, rinse, or wash mouth out for 5 minutes after taking the tablet.
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There can be variation in the licensing of different medicines containing the same drug. Forms available from special-order manufacturers include: oral solution Tablet Nervous system ▶Eldepryl (Orion Pharma (UK) Ltd) Selegiline hydrochloride 5 mg Eldepryl 5mg tablets | 100 tablet P £16.52 DT = £16.52 Selegiline hydrochloride 10 mg Eldepryl 10mg tablets | 100 tablet P £32.23 DT = £32.23 Oral lyophilisate EXCIPIENTS: May contain Aspartame ▶Zelapar (Teva UK Ltd) Selegiline hydrochloride 1.25 mg Zelapar 1.25mg oral lyophilisates sugar-free | 30 tablet P £43.16 DT = £43.16 Nausea and labyrinth disorders Nausea and labyrinth disorders Drug treatment Antiemetics should be prescribed only when the cause of vomiting is known because otherwise they may delay diagnosis, particularly in children. Antiemetics are unnecessary and sometimes harmful when the cause can be treated, such as in diabetic ketoacidosis, or in digoxin p. 116 or antiepileptic overdose. If antiemetic drug treatment is indicated, the drug is chosen according to the aetiology of vomiting. Antihistamines are effective against nausea and vomiting resulting from many underlying conditions. There is no evidence that any one antihistamine is superior to another but their duration of action and incidence of adverse effects (drowsiness and antimuscarinic effects) differ. The phenothiazines are dopamine antagonists and act centrally by blocking the chemoreceptor trigger zone. They are of considerable value for the prophylaxis and treatment of nausea and vomiting associated with diffuse neoplastic disease, radiation sickness, and the emesis caused by drugs such as opioids, general anaesthetics, and cytotoxics. Prochlorperazine p. 407, perphenazine, and trifluoperazine p. 408 are less sedating than chlorpromazine hydrochloride p. 402; severe dystonic reactions sometimes occur with phenothiazines, especially in children. Some phenothiazines are available as rectal suppositories, which can be useful in patients with persistent vomiting or with severe nausea; prochlorperazine can also be administered as a buccal tablet which is placed between the upper lip and the gum. Other antipsychotic drugs including haloperidol p. 404 and levomepromazine p. 460 are used for the relief of nausea and vomiting in terminal illness. Metoclopramide hydrochloride p. 452 is an effective antiemetic and its activity closely resembles that of the phenothiazines. Metoclopramide hydrochloride also acts directly on the gastro-intestinal tract and it may be superior to the phenothiazines for emesis associated with gastroduodenal, hepatic, and biliary disease. Domperidone p. 451 acts at the chemoreceptor trigger zone. It has the advantage over metoclopramide hydrochloride and the phenothiazines of being less likely to cause central effects such as sedation and dystonic reactions because it does not readily cross the blood-brain barrier. In Parkinson’s disease, domperidone [unlicensed in those weighing less than 35 kg] can be used to treat nausea caused by dopaminergic drugs. The MHRA and CHM have released important safety information and restrictions regarding the use of domperidone for nausea and vomiting in those weighing less than 35 kg, and a reminder of contra- indications. For further information, see Important safety information for domperidone. Granisetron p. 454 and ondansetron p. 455 are of value in the management of nausea and vomiting in patients receiving cytotoxics and in postoperative nausea and vomiting. Palonosetron p. 456 is licensed for prevention of nausea and vomiting associated with moderately or highly emetogenic cytotoxic chemotherapy. Palonosetron is also available in combination with netupitant, a neurokinin 1-receptor antagonist, for the prevention of acute and delayed nausea and vomiting associated with moderately emetogenic chemotherapy and highly emetogenic cisplatin- based chemotherapy. Dexamethasone p. 712 has antiemetic effects and it is used in vomiting associated with cancer chemotherapy. It can be used alone or with metoclopramide hydrochloride, prochlorperazine, lorazepam p. 355, or a 5HT3-receptor antagonist. Aprepitant p. 453, fosaprepitant p. 453, and rolapitant p. 454 are neurokinin 1-receptor antagonists. Aprepitant is licensed for the prevention of nausea and vomiting associated with highly and moderately emetogenic chemotherapy; fosaprepitant is licensed for the prevention of acute and delayed nausea and vomiting associated with highly emetogenic cisplatin-based chemotherapy and the prevention of nausea and vomiting associated with moderately emetogenic chemotherapy; rolapitant is licensed for the prevention of delayed nausea and vomiting associated with highly and moderately emetogenic chemotherapy. These drugs are given with dexamethasone and a 5HT3-receptor antagonist. For further information on the prevention of nausea and vomiting caused by chemotherapy, see Cytotoxic drugs p. 938. Nabilone p. 450 is a synthetic cannabinoid. g It can be considered as an add-on treatment for chemotherapy- induced nausea and vomiting unresponsive to optimised conventional antiemetics. h Vomiting during pregnancy Nausea in the first trimester of pregnancy is generally mild and does not require drug therapy. On rare occasions if vomiting is severe, short-term treatment with an antihistamine, such as promethazine, may be required. Prochlorperazine or metoclopramide hydrochloride are alternatives. If symptoms do not settle in 24 to 48 hours then specialist opinion should be sought. Hyperemesis gravidarum is a more serious condition, which requires regular antiemetic therapy, intravenous fluid and electrolyte replacement and sometimes nutritional support. Supplementation with thiamine p. 1141 must be considered in order to reduce the risk of Wernicke’s encephalopathy. Postoperative nausea and vomiting The incidence of postoperative nausea and vomiting depends on many factors including the anaesthetic used, and the type and duration of surgery. Other risk factors include female sex, non-smokers, a history of postoperative nausea and vomiting or motion sickness, and intraoperative and postoperative use of opioids. Therapy to prevent postoperative nausea and vomiting should be based on the assessed risk of postoperative nausea and vomiting in each patient. Drugs used include 5HT3-receptor antagonists, droperidol p. 460, dexamethasone, some phenothiazines (e.g. prochlorperazine), and antihistamines (e.g. cyclizine p. 449). A combination of two or more antiemetic drugs that have different mechanisms of action is often indicated in those at high risk of postoperative nausea and vomiting or where postoperative vomiting presents a particular danger (e.g. in some types of surgery). When a prophylactic antiemetic drug has failed, postoperative nausea and vomiting should be treated with one or more drugs from a different class. Motion sickness Antiemetics should be given to prevent motion sickness rather than after nausea or vomiting develop. The most effective drug for the prevention of motion sickness is hyoscine hydrobromide p. 458. The sedating antihistamines are slightly less effective against motion sickness, but are generally better tolerated than hyoscine. If a sedative effect is desired promethazine is useful, but generally a slightly less sedating antihistamine such as cyclizine or cinnarizine p. 457 is preferred. Domperidone, metoclopramide hydrochloride, 5HT3-receptor antagonists, and the phenothiazines (except the antihistamine phenothiazine promethazine) are ineffective in motion sickness. Other vestibular disorders Management of vestibular diseases is aimed at treating the underlying cause as well as treating symptoms of the balance disturbance and associated nausea and vomiting. Vertigo and nausea associated with Ménière’s disease and middle- ear surgery can be difficult to treat. Betahistine dihydrochloride p. 461 is an analogue of histamine and is claimed to reduce endolymphatic pressure by improving the microcirculation. Betahistine dihydrochloride is licensed for vertigo, tinnitus, and hearing loss associated with Ménière’s disease. A diuretic alone or combined with salt restriction may provide some benefit in vertigo associated with Ménière’s disease; antihistamines (such as cinnarizine p. 457), and phenothiazines (such as prochlorperazine p. 407) are also used. Where possible, prochlorperazine should be reserved for the treatment of acute symptoms. Nausea and vomiting associated with migraine For information on the use of antiemetics in migraine attacks, see Migraine p. 495. Other drugs used for Nausea and labyrinth disorders Paracetamol with metoclopramide, p. 497. Promethazine hydrochloride, p. 301 ANTIEMETICS AND ANTINAUSEANTS › ANTIHISTAMINES
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Avoid abrupt withdrawal.
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Patients or carers should be advised on how to administer selegiline hydrochloride oral lyophilisates. Driving and skilled tasks Drugs and driving Prescribers and other healthcare professionals should advise patients if treatment is likely to affect their ability to perform skilled tasks (e.g. driving). This applies especially to drugs with sedative effects; patients should be warned that these effects are increased by alcohol. General information about a patient’s fitness to drive is available from the Driver and Vehicle Licensing Agency at www.dvla.gov.uk. 2015 legislation regarding driving whilst taking certain drugs, may also apply to selegiline, see Drugs and driving under Guidance on prescribing p. 1.
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Initially 5 mg once daily for 2–4 weeks, then
First-line fragment. Read the complete Indications and Dose section above.
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1.25 mg once daily, dose to be taken before
First-line fragment. Read the complete Indications and Dose section above.
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