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|Selegiline Transdermal |
Drugs search, click the first letter of a drug name: | A | B | C | D | E | F | G | H | I | J | K | L | M | N | O | P | Q | R | S | T | U | V | W | X | Y | Z | 1 | 2 | 3 | 4 | 5 | 6 | 8 | 9 Home Selegiline TransdermalPronouncation: (se-LEJ-i-leen transdermal)Class: Antidepressant Trade Names: Mechanism of ActionPharmacologyPotentiation of monoamine neurotransmitter activity in the CNS resulting from inhibition of MAO activity is suspected. PharmacokineticsAbsorptionFollowing dermal application, 25% to 30% of the selegiline content is delivered systemically over 24 hr. The degree of absorption may be one-third higher than amounts of 6 to 12 mg per 24 hr. Because extensive first-pass metabolism occurs with oral administration, substantially higher exposure to selegiline and lower exposure to metabolites occur with transdermal dosing. DistributionPlasma protein binding is approximately 90%. MetabolismThe major enzymes involved with selegiline metabolism appear to be CYP2B6, CYP2C9, and CYP3A4/5, with CYP2A6 having a minor role. EliminationUrine and fecal elimination account for about 10% and 2%, respectively, of a dermal dose. At least 63% of the dose is not absorbed. Special PopulationsRenal Function ImpairmentNo adjustment of dermal dose is required with renal function impairment. Hepatic Function ImpairmentNo adjustment of dermal dose is required with moderate liver function impairment. Indications and UsageTreatment of major depressive disorder (MDD). ContraindicationsCoadministration with any of the following: analgesic agents (eg, tramadol, methadone, propoxyphene), bupropion, carbamazepine, cocaine or local anesthetics, cyclobenzaprine, dextromethorphan, dual serotonin and norepinephrine reuptake inhibitors (eg, venlafaxine), meperidine, mirtazapine, oral selegiline or other MAO inhibitors (eg, phenelzine), oxcarbazepine, SSRIs (eg, fluoxetine), St. John"s wort, sympathomimetic amines (eg, amphetamine), tricyclic antidepressants (eg, amitriptyline), vasoconstrictors (eg, pseudoephedrine). Patients with pheochromocytoma; hypersensitivity to any component of the product. Patients should not undergo elective surgery requiring general anesthetics. Discontinue selegiline transdermal at least 10 days prior to elective surgery. Dosage and AdministrationAdultsTransdermal Recommended starting and target dose is 6 mg per 24 hr. Based on clinical judgement, the dose may be increased in increments of 3 mg per 24 hr at intervals of no less than 2 wk (max, 12 mg per 24 hr). General Advice
Storage/StabilityStore at 68° to 77°F. Do not store outside sealed pouch. Drug InteractionsAnalgesics (eg, methadone, propoxyphene, tramadol), bupropion, carbamazepine, cocaine or local anesthetics, cyclobenzaprine, dextromethorphan, dual serotonin and norepinephrine reuptake inhibitors (eg, venlafaxine), mirtazapine, oral selegiline or other MAO inhibitors (eg, phenelzine), oxcarbazepine, St. John"s wort, SSRIs (eg, fluoxetine), sympathomimetic amines (eg, amphetamine), tricyclic antidepressants (eg, amitriptyline), vasoconstrictors (eg, pseudoephedrine)Coadministration with selegiline is contraindicated. BuspironeIncreased BP may occur. Drugs affecting monoamine activity (eg, amphetamines, meperidine, pentazocine, SSRIs, tricyclic antidepressants)Severe, life-threatening toxicity, including serotonin syndrome (eg, rigidity, muscle twitching, mental status change, autonomic instability), may occur. General anestheticsPatients should not undergo elective surgery requiring general anesthetics; discontinue selegiline transdermal at least 10 days prior to elective surgery. Oral contraceptivesSelegiline plasma levels may be elevated, increasing the pharmacologic and adverse effects. Tyramine-containing nutritional supplementsShould be avoided. Laboratory Test InteractionsNone well documented. Adverse ReactionsCardiovascularOrthostatic hypotension (10%); low systolic BP (3%); hypertension (at least 1%). CNSHeadache (18%); insomnia (12%); abnormal thinking, agitation, amnesia, paresthesia (at least 1%). DermatologicRash (4%); acne, pruritus, sweating (at least 1%). EENTPharyngitis (3%); taste perversion, tinnitus (at least 1%). GIDiarrhea (9%); dry mouth (8%); dyspepsia (4%); anorexia, constipation, flatulence, gastroenteritis, vomiting (at least 1%). GenitourinaryAbnormal ejaculation (1%); dysmenorrhea, metrorrhagia, urinary frequency, UTI (at least 1%). Hematologic-LymphaticEcchymosis (at least 1%). LocalApplication site reaction (at least 2%). Metabolic-NutritionalWeight gain (5%); peripheral edema (at least 1%). MusculoskeletalMyalgia, pathological fracture (at least 1%). RespiratorySinusitis (3%); bronchitis, increased cough (at least 1%). MiscellaneousChest pain, neck pain (at least 1%). Precautions
PregnancyCategory C . LactationUndetermined. ChildrenSafety and efficacy not established. ElderlyNo overall differences in efficacy have been noted between elderly and younger patients. Dietary modificationsAvoid food and beverages rich in tyramine for patients taking selegiline 9 mg per 24 hr and 12 mg per 24 hr. Hypertensive crisisMay be a risk in patients taking amine-containing medications or tyramine foods if the dose of selegiline is exceeded or if plasma levels are elevated. Mania/HypomaniaActivation may occur; use with caution in patients with history of mania. Screening for bipolar disorderPrior to initiating treatment, adequately screen patients with depressive symptoms to determine risk of bipolar disorder. OverdosageSymptomsAgitation, coma, convulsions, cool clammy skin, death, diaphoresis, dizziness, drowsiness, faintness, hallucinations, hyperactivity, hyperpyrexia, hypertension, hypotension, irritability, opisthotonos, precordial pain, rapid and irregular pulse, respiratory depression and failure, severe headache, trismus, vascular collapse. Patient Information
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