Overview
11 DESCRIPTION Tranylcypromine sulfate, the active ingredient of Tranylcypromine Tablets, USP, is a non-hydrazine MAOI. The chemical name is (±)- trans -2-phenylcyclopropylamine sulfate (2:1). The molecular formula is (C 9 H 11 N) 2 ∙H 2 SO 4 and its molecular weight is 364.46. The structural formula is: Tranylcypromine film-coated tablets are intended for oral administration.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism of action of tranylcypromine tablets as an antidepressant is not fully understood, but is presumed to be linked to potentiation of monoamine neurotransmitter activity in the central nervous system (CNS) resulting from its irreversible inhibition of the enzyme monoamine oxidase (MAO). 12.2 Pharmacodynamics Although tranylcypromine is eliminated in 24 hours, recovery MAO activity takes up to 3 to 5 days [see Warnings and Precautions (5.9) ] .
Indications
- 1 INDICATIONS AND USAGE Tranylcypromine tablets are indicated for the treatment of major depressive disorder (MDD) in adult patients who have not responded adequately to other antidepressants. Tranylcypromine tablets are not indicated for the initial treatment of MDD due to the potential for serious adverse reactions and drug interactions, and the need for dietary restrictions [see Contraindications (4) , Warnings and Precautions (5) , and Drug Interactions (7) ] .
Common Doses
- 30 mg
- 10 mg
- 60 mg
Dosage
2 DOSAGE AND ADMINISTRATION • Recommended daily dosage is 30 mg in divided doses ( 2.1 ) • If no adequate response, increase dosage in increments of 10 mg per day every 1 to 3 weeks to a maximum dosage of 30 mg twice daily (60 mg per day). Consider more gradual dosage increases in patients at risk for hypotension ( 2.1 ) • Consider discontinuing tranylcypromine tablets therapy gradually because of the risk for withdrawal effects ( 2.3 , 5.8 , 9.3 ) • Switching from or to other MAOIs or other antidepressants: See full prescribing information for instructions ( 2.2 , 7.1 ) 2.
Black Box Warning
WARNING: SUICIDAL THOUGHTS AND BEHAVIORS and HYPERTENSIVE CRISIS WITH SIGNIFICANT TYRAMINE USE WARNING: SUICIDAL THOUGHTS AND BEHAVIORS and HYPERTENSIVE CRISIS WITH SIGNIFICANT TYRAMINE USE See full prescribing information for complete boxed warning. • Increased risk of suicidal thoughts and behavior in pediatric and young adult patients taking antidepressants. Closely monitor all antidepressant-treated patients for clinical worsening and emergence of suicidal thoughts and behaviors. Tranylcypromine tablets are not approved for use in pediatric patients. ( 5.1 , 8.
Contraindications
- 4 CONTRAINDICATIONS • Concomitant use or use in rapid succession with other MAOIs; selective serotonin reuptake inhibitors; serotonin and norepinephrine reuptake inhibitors; tricyclic antidepressants; sympathomimetic drugs; and numerous other drugs. See Full Prescribing Information for the full list of contraindicated products ( 4.1 , 7.1 ) • Pheochromocytoma, other catecholamine-releasing paraganglioma ( 4.2 ) 4.1 Combination with Certain Drugs Concomitant use of tranylcypromine tablets or use in rapid succession with the products in Table 1 is contraindicated.
Side Effects
- 6 ADVERSE REACTIONS The following adverse reactions are described in greater detail in other sections: • Suicidal thoughts and behaviors [see Warnings and Precautions (5.1) ] • Hypertensive crisis and hypertension [see Warnings and Precautions (5.2) ] • Serotonin syndrome [see Warnings and Precautions (5.3) ] • Activation of mania/hypomania [see Warnings and Precautions (5.4) ] • Hypotension [see Warnings and Precautions (5.5) ] • Hypotension and hypertension during anesthesia and perioperative care [see Warnings and Precautions (5.
Interactions
- 7 DRUG INTERACTIONS See Full Prescribing Information for a list of products, foods and beverages that can interact with tranylcypromine tablets ( 7 ) 7.1 Clinically-Significant Drug Interactions Tables 3 and 4 lists drug classes and individual products, respectively, with a potential for interaction with tranylcypromine tablets, describes the predominant observed or anticipated risks, and provides advice on concomitant use.