Nitrate Vasodilator

Rectiv

Approved 21 Jun 2011Intra-analOintment

Indications

RECTIV ® (nitroglycerin) Ointment 0.4% is indicated for the treatment of moderate to severe pain associated with chronic anal fissure. RECTIV is a nitrate vasodilator indicated for the treatment of moderate to severe pain associated with chronic anal fissure ( 1 ).

Contraindications

Use of PDE5 inhibitors (e.g. sildenafil, vardenafil and tadalafil) as these are shown to potentiate the hypotensive effects of organic nitrates. ( 4.1 ). Severe anemia ( 4.2 ) Increased intracranial pressure ( 4.3 ) Known hypersensitivity to nitroglycerin, other nitrates and nitrites, or any components of the ointment. ( 4.4 )

4.1 PDE5 inhibitor use Administration of RECTIV is contraindicated in patients who are using a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), such as sildenafil, vardenafil, and tadalafil, as these are shown to potentiate the hypotensive effects of organic nitrates [see DRUG INTERACTIONS ( 7.1 ) ] .

4.2 Severe anemia RECTIV is contraindicated in patients with severe anemia.

4.3 Increased intracranial pressure RECTIV is contraindicated in patients with increased intracranial pressure.

4.4Hypersensitivity

RECTIV is contraindicated in patients who have shown hypersensitivity to it or to other nitrates or nitrites. Skin reactions consistent with hypersensitivity have been observed with organic nitrates.

Warnings and precautions

Cardiovascular Disorders: Venous and arterial dilatation as a consequence of nitroglycerin treatment can result in hypotension. Exercise caution when treating patients with any of the following conditions: blood volume depletion, existing hypotension, cardiomyopathies, congestive heart failure, acute myocardial infarction, or poor cardiac function for other reasons ( 5.1 ). Headache: Nitroglycerin produces dose-related headaches which may be severe ( 5.2 ) 5. 1 Cardi ovascular disorders Venous and arterial dilatation as a consequence of nitroglycerin treatment including RECTIV, can decrease venous blood returning to the heart and reduce arterial vascular resistance and systolic pressure.

At a glance

Brand name: Rectiv
Active substance: nitroglycerin
Pharmacologic class: Nitrate Vasodilator
Route: Intra-anal
Dosage form: Ointment
Applicant: Abbvie
Status: Discontinued
FDA approval: 21 Jun 2011
Application: NDA021359-001

Contraindications

4.2 Severe anemia RECTIV is contraindicated in patients with severe anemia.

4.3 Increased intracranial pressure RECTIV is contraindicated in patients with increased intracranial pressure.

4.4Hypersensitivity

RECTIV is contraindicated in patients who have shown hypersensitivity to it or to other nitrates or nitrites. Skin reactions consistent with hypersensitivity have been observed with organic nitrates.

Warnings and precautions

Interactions

PDE5 inhibitors: potentiation of hypotensive effects of organic nitrates; concomitant use is contraindicated. ( 4.1 , 7.1 ) Antihypertensives: possible additive hypotensive effects. ( 7.2 ) Aspirin: increased nitroglycerin levels. ( 7.3 ) Tissue-type Plasminogen Activator (t-PA): decreased thrombolytic effect. ( 7.4 ) Heparin: anticoagulant effect of heparin may be reduced. Monitor APTT. ( 7.5 ) Ergotamine: increased bioavailability of ergotamine.

( 7.6 ) Alcohol: Additive vasodilatory effects to nitroglycerin. Consumption of alcohol should be avoided. ( 7.7 )

7.1 PDE5 inhibitors Phosphodiesterase type 5 (PDE5) inhibitors such as sildenafil, vardenafil, and tadalafil have been shown to potentiate the hypotensive effects of organic nitrates. The time course of the interaction appears to be related to the half-life of the PDE5 inhibitor, however, the dose dependence of this interaction has not been studied. Use of RECTIV within a few days of PDE5 inhibitors is contraindicated.

7.2Antihypertensives

Patients receiving antihypertensive drugs, beta-adrenergic blockers, and other nitrates should be observed for possible additive hypotensive effects when using RECTIV. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with RECTIV in patients with angina pectoris, additional hypotensive effects may occur.

7.3Aspirin Coadministration

of aspirin (at doses between 500 mg and 1000 mg) and nitroglycerin has been reported to result in increased nitroglycerin maximum concentrations by as much as 67% and AUC by 73% when administered as a single dose. The pharmacological effects of RECTIV may be enhanced by concomitant administration of aspirin.

7.4Tissue-type Plasminogen Activator (t-PA)

Intravenous administration of nitroglycerin decreases the thrombolytic effect of tissue-type plasminogen activator (t-PA). Plasma levels of t-PA are reduced when coadministered with nitroglycerin. Therefore, caution should be observed in patients receiving RECTIV during t-PA therapy.

7.5Heparin Although

an interaction has been reported between intravenous heparin and intravenous nitroglycerin (resulting in a decrease in the anticoagulant effect of heparin), the data are not consistent. If patients are to receive intravenous heparin and RECTIV concurrently, the anticoagulation status of the patient must be checked.

7.6Ergotamine

Oral administration of nitroglycerin markedly decreases the first-pass metabolism of dihydroergotamine and consequently increases its oral bioavailability. Ergotamine is known to precipitate angina pectoris. Therefore the possibility of ergotism in patients receiving RECTIV should be considered.

7.7Alcohol

The vasodilating effects of nitroglycerin have been shown to be additive to the effects observed with alcohol.

Rectiv

Indications

Contraindications

4.4Hypersensitivity

Warnings and precautions

At a glance

Two medicines in one question?

Rectiv

Indications

Contraindications

4.4Hypersensitivity

Warnings and precautions

At a glance

Two medicines in one question?

Interactions

7.2Antihypertensives

7.3Aspirin Coadministration

7.4Tissue-type Plasminogen Activator (t-PA)

7.5Heparin Although

7.6Ergotamine

7.7Alcohol

Pregnancy and breastfeeding

8.1Pregnancy Risk Summary

Adverse reactions

Composition

Official product information