nitroglycerin rectal (Rx)Brand and Other Names:Rectiv

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

ointment, intra-anal

  • 0.4% (4mg nitroglycerin/1g of ointment)
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Chronic Rectal Fissure Pain

Indicated for treatment of moderate-to-severe pain associated with chronic anal fissures; consider use if conservative treatment for acute symptoms of anal fissure fails

Cover finger with plastic-wrap, disposable surgical glove or a finger cot and measure 1-inch (375 mg of ointment equivalent to 1.5 mg of nitroglycerin) length of ointment using dosing line provided with packaging

The covered finger is then gently inserted into the anal canal no further than to the first finger joint and applied circumferentially to the anal canal

If this cannot be achieved due to pain, application of the ointment should be made directly to the outside of the anus

May be applied intra-anally q12h until pain abates, not to exceed treatment duration of 3 weeks

Storage

Do not store above 25°C

Do not freeze

Keep the tube tightly closed

Safety and efficacy not established

Clinical studies did not include sufficient numbers of individuals aged 65 yr or older to determine whether they respond differently from younger individuals

Clinical data from the published literature indicate that the elderly demonstrate increased sensitivity to nitrates, which may be therapeutic but also manifest by more frequent or severe hypotension and related dizziness or fainting

Increased sensitivity may reflect the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy common in elderly individuals

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Interactions

Interaction Checker

nitroglycerin rectal and

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined

            Headache

            Dizziness

            Lightheadedness

            Nausea

            Vomiting

            Hypotension, including orthostatic hypotension

            Allergic reactions, flushing, and application site reactions (including drug rash and exfoliative dermatitis)

            Methemoglobinemia may occur with organic nitrates, particularly in the setting of overdose

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            Warnings

            Contraindications

            Hypersensitivity to nitroglycerin or to any of the excipients or idiosyncratic reactions to other organic nitrates

            Use within a few days of selective PDE-5 inhibitors (eg, sildenafil, tadalafil, vardenafil); as these may potentiate hypotensive effects of organic nitrates; the time course of the interaction appears to be related to the PDE-5 inhibitor half-life

            Increased intracranial pressure (eg, head trauma, cerebral hemorrhage) or inadequate cerebral circulation

            Severe anemia

            Cautions

            Caution with existing cardiovascular disorders; venous and arterial dilatation may occur and decrease venous blood return to the heart and reduce arterial vascular resistance and systolic pressure

            Caution with blood volume depletion, existing hypotension, cardiomyopathies, CHF, acute MI, or poor cardiac function for other reasons

            Headache: Nitroglycerin produces dose-related headaches which may be severe

            Additive hypotensive effects may occur when coadministration with nitric oxide (NO) donors (eg, long-acting nitroglycerin, isosorbide dinitrate, isosorbide mononitrate, amyl nitrite, butyl nitrite), antihypertensive drugs, beta-adrenergic blockers, and calcium channel blockers

            Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects

            Coadministration with aspirin may increase nitroglycerin maximum serum concentration and AUC

            Alcohol may enhance nitroglycerin’s vasodilating effects

            Avoid use in patients with hypertrophic cardiomyopathy

            Caution when coadministration with t-PA, heparin, and ergotamine

            May precipidate or aggravate intracranial pressure

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: Unknown whether distributed in breast milk/use caution

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Organic nitrate; nitric oxide released from nitroglycerin elicits internal anal sphincter relaxation; reduces sphincter tone and resting intra-anal pressure

            The smooth muscle relaxation is a result of guanylate cyclase activation and resulting increased cyclic GMP in smooth muscle and other tissues causing myosin dephosphorylation; this ultimately results in vasodilatation

            Hypertonicity of the internal but not the external anal sphincter is a predisposing factor in the formation of anal fissures and associated spasm; hypertonicity of the IAS may thereby decrease blood flow and cause ischemia to this region

            Absorption

            Bioavailability: 50% (with application of 0.75 mg dose of 0.2% ointment)

            Distribution

            Protein Bound: 60% (IV)

            Vd: 3 L/kg (IV)

            Metabolism

            Metabolized by liver reductase enzyme to glycerol di- and mononitrate metabolites and ultimately to glycerol and organic nitrate; extrahepatic metabolism include red blood cells and vascular walls

            Enzyme substrate, inhibitor, inducer Metabolites: Inorganic nitrate and 1,2 and 1,3-dinitroglycerols (partially active); the dinitrates are further metabolized to nonvasoactive mononitrates and ultimately to glycerol and carbon dioxide

            Elimination

            Half-life (mean): 2-3 minutes

            Total body clearance: 13.6 L;/min

            Metabolism is primary route of drug elimination

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            Formulary

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
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