Nitromak Retard Actions

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Actions of Nitromak Retard in details

The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.

Description: Nitromak Retard forms free radical nitric oxide (NO), which stimulates guanylate cyclase in the vascular smooth muscle cells resulting in relaxation of smooth muscles. It reduces cardiac oxygen demand by decreasing preload and may modestly reduce afterload, dilates coronary arteries and improves collateral flow to ischaemic regions. It also decreases sphincter tone and intra-anal pressure when administered rectally.

Onset: W/in 1-3 min (sublingual, buccal); w/in 30-60 min (transdermal, topical); w/in 1-2 min (IV).

Duration: Approx 30-60 min (sublingual); 3-5 hr (modified-release buccal tab); 24 hr (transdermal); up to 12 hr (topical); approx 3-5 min (IV).


Absorption: Rapidly absorbed from oral mucosa; well absorbed from the GI tract and through the skin. Bioavailability: <100%.

Distribution: Widely distributed; taken up by RBCs and smooth muscles cells of the blood vessels. Volume of distribution: Approx 3 L/kg. Plasma protein binding: 60%.

Metabolism: Rapidly metabolised in the liver by glutathione-organic nitrate reductase to form di- and mononitrate metabolites; undergoes hydrolysis in the plasma.

Excretion: Via urine (as inactive metabolites). Plasma half-life: Approx 3 min (Nitromak Retard); approx 30-60 min (dinitrate metabolites).

How should I take Nitromak Retard?

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended. Keep this medicine on hand at all times in case of an angina attack. Get your prescription refilled before you run out of medicine completely.

Nitromak Retard is usually taken at the first sign of chest pain. If possible, try to rest or stay seated when you use this medication. Nitromak Retard can cause dizziness or fainting.

You may use Nitromak Retard sublingual within 5 to 10 minutes before an activity you think might cause chest pain. Follow your doctor's instructions.

If you use Nitromak Retard sublingual spray to treat an angina attack: At the first sign of an attack, apply the spray directly on or under your tongue. Close your mouth after each spray. Do not inhale the spray. Do not shake the spray before or during use. You may use additional sprays every 5 minutes, but not more than 3 sprays in 15 minutes.

The Nitromak Retard sublingual tablet should be placed under your tongue and allowed to dissolve slowly. Do not chew or swallow it. You may use additional tablets every 5 minutes, but not more than 3 tablets in 15 minutes.

Seek emergency medical attention if your chest pain gets worse or lasts more than 5 minutes, especially if you have trouble breathing or feel weak, dizzy, or nauseated, or lightheaded.

You may feel a slight burning or stinging in your mouth when you use this medicine. However, this sensation is not a sign of how well the medication is working. Do not use more medication just because you do not feel a burning or stinging.

Do not crush, chew, break, or open an extended-release capsule. Swallow it whole.

This medicine can cause unusual results with certain medical tests. Tell any doctor who treats you that you are using Nitromak Retard.

If you take Nitromak Retard on a regular schedule to prevent angina, do not stop taking it suddenly or you could have a severe attack of angina.

Store the tablets in the glass container at room temperature, away from moisture and heat. Keep the bottle tightly closed when not in use.

Keep the spray away from open flame or high heat, such as in a car on a hot day. The canister may explode if it gets too hot.

Nitromak Retard administration

Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.

IV: Prepare in glass bottles, EXCEL or PAB containers. Adsorption occurs to soft plastic (eg, PVC); use administration sets intended for Nitromak Retard. Avoid in-line IV filters that adsorb Nitromak Retard. Administer via infusion pump.

Intra-anal ointment: Using a finger covering (eg, plastic wrap, surgical glove, finger cot), place finger beside 1 inch measuring guide on the box and squeeze ointment the length of the measuring line directly onto covered finger. Insert ointment into the anal canal using the covered finger up to first finger joint (do not insert further than the first finger joint) and apply ointment around the side of the anal canal. If intra-anal application is too painful, may apply the ointment to the outside of the anus. Wash hands following application.

ER capsule: Swallow whole. Do not chew, break, or crush. Administer with a full glass of water.

Bariatric surgery: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate.

Topical ointment and transdermal formulations are available. If safety and efficacy of Nitromak Retard can be effectively monitored, no change in formulation or administration is required after bariatric surgery; however, selection of ointment, transdermal, or alternative therapy should be considered in high-risk patients.

Sublingual powder: Empty the contents of packet under the tongue, close mouth, and breathe normally. Allow powder to dissolve without swallowing. Do not rinse or spit for 5 minutes after dosing.

Sublingual tablet: Do not chew, crush, or swallow sublingual tablet. Place under tongue and allow to dissolve. Alternately, may be placed in the buccal pouch. May take small sip of water prior to placing tablet under the tongue to aid dissolution.

Topical ointment: Wash hands prior to and after use. Application site should be clean, dry, and hair-free. Apply to chest or back with the applicator or dose-measuring paper. Spread in a thin layer over a 2.25 x 3.5 inch area. Do not rub into skin. Tape applicator into place.

Sympathomimetic vasopressors extravasation injury (alternative to phentolamine) (off-label use): Stop vesicant infusion immediately and disconnect IV line (leave needle/cannula in place); gently aspirate extravasated solution from the IV line (do NOT flush the line); remove needle/cannula; elevate extremity. Apply Nitromak Retard ointment as a thin ribbon to site of ischemia (Reynolds 2014; Wong 1992). May also apply dry warm compresses (Hurst 2004; Reynolds 2014).

Topical patch, transdermal: Application site should be clean, dry and hair-free. Remove patch after 12 to 14 hours. Rotate patch sites. Dispose of any used of unused patches by folding adhesive ends together, replace in pouch or sealed container and discard properly in trash, away from children and pets.

Translingual spray: Do not shake container. Prior to initial use, the pump must be primed by spraying 5 times (Nitrolingual) or 10 times (Nitromist) into the air. Priming sprays should be directed away from patient and others. Release spray onto or under tongue. Close mouth immediately after administration; do not inhale spray. Do not expectorate or rinse the mouth for 5 to 10 minutes following administration. Content of the container should be checked periodically; when the container is held upright, the end of the pump should be covered by the fluid in the bottle or the remaining sprays will not deliver the intended dose. If pump is unused for 6 weeks, a single priming spray (Nitrolingual) or 2 priming sprays (Nitromist) should be completed. If pump is unused for 3 months, re-prime with up to 5 sprays (Nitrolingual).

Nitromak Retard pharmacology

Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.

Mechanism Of Action

Nitromak Retard forms free radical nitric oxide (NO), which activates guanylate cyclase, resulting in an increase of guanosine 3',5'-monophosphate (cyclic GMP) in smooth muscle and other tissues. This leads to dephosphorylation of myosin light chains, which regulates the contractile state in smooth muscle and results in vasodilatation.


The principal pharmacological action of Nitromak Retard is relaxation of vascular smooth muscle. Intraanal application of Nitromak Retard reduces sphincter tone and resting intra-anal pressure.



In six healthy subjects, the average absolute bioavailability of Nitromak Retard applied to the anal canal as a 0.2% w/w ointment was approximately 50% of the 0.75 mg Nitromak Retard dose.


The volume of distribution of Nitromak Retard following intravenous administration is about 3 L/kg. At plasma concentrations between 50 and 500 ng/mL, the binding of Nitromak Retard to plasma proteins is approximately 60%, while that of 1,2- and 1,3-dinitroglycerin is 60% and 30%, respectively.


Nitromak Retard is metabolized by a liver reductase enzyme to glycerol di- and mononitrate metabolites and ultimately to glycerol and organic nitrate. Known sites of extrahepatic metabolism include red blood cells and vascular walls. In addition to Nitromak Retard, the two major metabolites, 1,2- and 1,3- dinitroglycerols are found in plasma. The contribution of metabolites to the relaxation of the internal anal sphincter is unknown. The dinitrates are further metabolized to nonvasoactive mononitrates and ultimately to glycerol and carbon dioxide.


Metabolism is the primary route of drug elimination. Nitromak Retard plasma concentrations decrease rapidly with a mean elimination half-life of two to three minutes. Half-life values range from 1.5 to 7.5 minutes. Clearance (13.6 L/min) greatly exceeds hepatic blood flow.

Clinical Studies

Nitromak Retard ointment was evaluated in a 3-week double-blind, randomized, multi-center, placebocontrolled study. Patients with a painful chronic anal fissure for at least 6 weeks and moderate or severe pain prior to treatment ( ≥ 50 mm on the 100mm visual analog scale, VAS) were randomized to receive 0.4% (1.5mg) Nitromak Retard or placebo ointment applied to the anal canal every 12 hours. Pain as assessed by the change in VAS from baseline to Days 14-18 was lower in patients receiving 0.4% ointment compared to placebo. The mean change from baseline was 44mm for Nitromak Retard and 37mm for placebo. The difference in the mean change in pain between Nitromak Retard and placebo was -7.0mm (95% Confidence Interval: -13.6 to -0.4mm).


  1. DailyMed. "NITROGLYCERIN: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". (accessed September 17, 2018).
  2. NCIt. "Nitroglycerin: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". (accessed September 17, 2018).
  3. EPA DSStox. "Trinitroglycerin: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". (accessed September 17, 2018).


The results of a survey conducted on for Nitromak Retard are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Nitromak Retard. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

User reports

2 consumers reported administration

When best can I take Nitromak Retard, on an empty stomach, before or after food? website users have also released a report stating that Nitromak Retard should be taken With a meal. In any case, this may not be the right description on how you ought to take this Nitromak Retard. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Nitromak Retard can be taken.
With a meal1
Empty stomach1

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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