Rectiv topical

Name: Rectiv topical

Introduction

Organic nitrate; vasodilating agent.1

Uses for Rectiv

Chronic Anal Fissure

Intra-anal treatment of moderate to severe pain associated with chronic anal fissure.1 3 6 7 8 9

Chronic anal fissure is thought to be related to sustained high resting anal sphincter tone and associated anodermal ischemia.7 Lateral internal sphincterotomy generally has been used to treat anal fissures that do not respond to conservative therapy (e.g., sitz baths, increased dietary fiber); however, minor incontinence, which may be persistent, may develop after surgery.3 5 7 Botulinum toxin type A injections or topical therapy with nitrates (e.g., nitroglycerin rectal ointment) or calcium-channel blocking agents (e.g., diltiazem gel, not commercially available in US) has been used to reduce anal sphincter tone and circumvent potential complications of surgery.3 5 9

Cautions for Rectiv

Contraindications

  • Known hypersensitivity to nitroglycerin, other nitrates or nitrites, or any ingredient in the formulation.1

  • Concomitant or recent (within a few days) treatment with selective phosphodiesterase type 5 (PDE5) inhibitors (e.g., sildenafil, tadalafil, vardenafil).1

  • Severe anemia or increased intracranial pressure.1

Warnings/Precautions

Sensitivity Reactions

Flushing, allergic reactions, and application site reactions (including drug rash and exfoliative dermatitis) reported rarely.1

Cardiovascular Effects

May cause venous and arterial dilation, which can decrease venous blood returning to the heart and reduce arterial vascular resistance and systolic pressure.1

Use with caution in patients with blood volume depletion, hypotension, cardiomyopathies, CHF, acute MI, or poor cardiac function; monitor cardiovascular status and clinical condition in such patients.1

More pronounced adverse cardiovascular effects likely in geriatric patients.1

Risk of transient lightheadedness, occasionally related to BP changes.1 Hypotension (including orthostatic hypotension), in some cases requiring discontinuance of nitroglycerin ointment, reported infrequently.1

Headache

Risk of dose-related headaches, which may be severe; headaches typically are of short duration and respond to analgesics (e.g., acetaminophen).1 8 Tolerance occurs but headache may recur after each dose.1 8 Prophylactic acetaminophen recommended by some clinicians.3

Specific Populations

Pregnancy

Category C.1

Lactation

Not known whether nitroglycerin is distributed into milk.1 Caution if used in nursing women.1

Pediatric Use

Safety and efficacy not established in pediatric patients <18 years of age.1

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.1

Increased sensitivity to nitrates (e.g., more frequent or severe hypotension and related dizziness or fainting) reported in geriatric patients; may be related to higher frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy.1

Common Adverse Effects

Headache,1 6 7 dizziness.1 6

Interactions for Rectiv

Specific Drugs

Drug

Interaction

Comments

Alcohol

Additive vasodilating effects, possibly resulting in hypotension1

Avoid concomitant use2

Aspirin

Possible increase in nitroglycerin concentrations and pharmacologic effects1

β-Adrenergic blocking agents

Possible additive hypotensive effects1

Monitor for possible additive effects (e.g., orthostatic hypotension)1

Calcium-channel blocking agents

Possible additive hypotensive effects1

Monitor for possible additive effects (e.g., orthostatic hypotension)1

Ergot alkaloids (e.g., dihydroergotamine, ergotamine)

Possible reduced first-pass metabolism and increased bioavailability of dihydroergotamine; may result in ergotism1

Ergotamine is known to precipitate angina pectoris1

Consider possibility of ergotism if used concomitantly1

Heparin

Possible decreased anticoagulant effect of IV heparin1

Monitor anticoagulation status if used concomitantly1

Hypotensive agents

Possible additive hypotensive effects1

Monitor for possible additive effects (e.g., orthostatic hypotension)1

Nitrates

Possible additive hypotensive effects1

Monitor for possible additive effects (e.g., orthostatic hypotension)1

PDE5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)

Potentiated hypotensive effects of organic nitrates1

Use of nitroglycerin ointment within a few days of PDE5 inhibitors is contraindicated1

Tissue-type plasminogen activator (t-PA)

Possible reduced plasma concentrations and thrombolytic effects of t-PA1

Use concomitantly with caution1

Actions

  • Principal pharmacologic property is relaxation of vascular smooth muscle, resulting in generalized vasodilation.1

  • Nitroglycerin forms free radical nitric oxide, which activates guanylate cyclase; activation of guanylate cyclase results in an increase of guanosine-3′,5′-monophosphate (cyclic GMP) in smooth muscle and other tissues, leading to dephosphorylation of myosin light chains and vasodilation.1

  • Intra-anal application of nitroglycerin reduces sphincter tone and resting intra-anal pressure.1 4 5 7 The reduction in anal pressure may result in increased anal blood flow.4 7

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