Nizozole

Nizozole Uses, Dosage, Side Effects, Food Interaction and all others data.

Nitroprusside a powerful vasodilator relaxes the vascular smooth muscle and produce consequent dilatation of peripheral arteries and veins. Other smooth muscle (e.g., uterus, duodenum) is not affected. Sodium nitroprusside is more active on veins than on arteries.

One molecule of sodium nitroprusside is metabolized by combination with hemoglobin to produce one molecule of cyanmethemoglobin and four CN- ions; methemoglobin, obtained from hemoglobin, can sequester cyanide as cyanmethemoglobin; thiosulfate reacts with cyanide to produce thiocyanate; thiocyanate is eliminated in the urine; cyanide not otherwise removed binds to cytochromes. Cyanide ion is normally found in serum; it is derived from dietary substrates and from tobacco smoke. Cyanide binds avidly (but reversibly) to ferric ion (Fe+++), most body stores of which are found in erythrocyte methemoglobin (metHgb) and in mitochondrial cytochromes. When CN is infused or generated within the bloodstream, essentially all of it is bound to methemoglobin until intraerythrocytic methemoglobin has been saturated. Once activated to NO, it activates guanylate cyclase in vascular smooth muscle and increases intracellular production of cGMP. cGMP stimulates calcium movement from the cytoplasm to the endoplasmic reticulum and reduces calcium available to bind with calmodulin. This eventually leads to vascular smooth muscle relaxation and vessel dilatation.

Trade Name Nizozole
Generic Sodium Nitroprusside Dihydrate
Weight 2%w/w
Type Cream
Therapeutic Class Vasodilator antihypertensive drugs
Manufacturer Ambrosia Pharmaceuticals
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am
Nizozole
Nizozole

Uses

Sodium nitroprusside is used for the immediate reduction of blood pressure of adult and pediatric patients in hypertensive crises. Concomitant longer-acting antihypertensive medication should be administered so that the duration of treatment with sodium nitroprusside can be minimized. Sodium nitroprusside is also used for producing controlled hypotension in order to reduce bleeding during surgery. This is also used for the treatment of acute congestive heart failure.

Dosage

Nizozole dosage

Intravenous Hypertensive crisis:

  • Adult: For patients not receiving any antihypertensives, initially 0.3-1.5 mcg/kg/ min, adjust gradually according to response. Usual range 0.5-6 mcg/kg/min. Lower doses should be used in patients receiving antihypertensives. Max rate: 8 mcg/kg/min, discontinue infusion if there is no response after 10 min. May continue for a few hr if there is response. Introduce oral antihypertensive as soon as possible.
  • Child: Initially, 250-500 nanograms/kg/min, rate may be repeatedly doubled at intervals of 15-20 min until the desired effect is achieved or treatment is judged ineffective. Max rate: 6 mcg/kg/min.
  • Elderly: Lower doses may be required.

Induction of hypotension during anaesthesia :

  • Adult: Recommended max dose: 1.5 mcg/kg/min.

Heart failure:

  • Adult: Intially 10-15 mcg/min, may increase by 10-15 mcg/min every 5-10 min according to response; usual range 10-200 mcg/min. Max: 280 mcg/min.

Side Effects

Bradyarrhythmia, hypotension, palpitations, tachyarrhythmia Apprehension, restlessness, confusion, dizziness, headache, somnolence Rash, sweating, Thyroid suppression, Injection site irritation, Muscle twitch, oliguria, renal azotemia, Cardiac dysrhythmia, hemorrhage, decreased platelet aggregation, excessive hypotensive response, Raised intracranial pressure, Metabolic acidosis, Bowel obstruction, Methemoglobinemia, Cyanide poisoning, Thiocyanate toxicity

Precaution

Hypothyroidism, renal and hepatic impairment, ischaemic heart disease, impaired cerebral circulation, elderly. Monitor blood thiocyanate concentration if treatment is longer than 3 days and should not exceed 100 mcg/ml. Monitor acid-base balance, venous oxygen concentration and BP. Caution to avoid extravasation. To be diluted with sterile dextrose 5% solution before infusion. Avoid sudden withdrawal. Leber's optic atrophy, low plasma-cobalamin concentrations, impaired pulmonary function. Pregnancy and lactation.

Interaction

Additive effect when used with other antihypertensives. May prolong the fibrinolytic activity of alteplase. Risk of severe hypotension if used with phosphodiesterase inhibitors. May reduce serum digoxin levels.

Pregnancy & Breastfeeding use

Pregnancy Category C. There are no adequate, well-controlled studies of Sodium Nitroprusside in either laboratory animals or pregnant women. It is not known whether Sodium Nitroprusside can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity. Sodium Nitroprusside should be given to a pregnant woman only if clearly needed.

Nursing Mothers: It is not known whether sodium nitroprusside and its metabolites are excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from sodium nitroprusside, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

Sodium stibogluconate is exceedingly toxic to veins. One of the practical problems is that after a few doses it can become exceedingly difficult to find a vein in which to inject the drug. The insertion of a PICC does not prevent the problem and can instead exacerbate it: the entire vein along the course of the PICC line can become inflamed and thrombose. Large doses of sodium stibogluconate are often administered as dilute solutions.

Pancreatitis is a common deleterious effect of the drug, and the serum amylase or lipase should be monitored twice weekly; there is no need to stop treatment if the amylase remains less than four times the upper limit of normal; if the amylase rises above the cut-off, then treatment should be interrupted until the amylase falls to less than twice the upper limit of normal, whereupon treatment can be resumed. Cardiac conduction disturbances are less common, but ECG monitoring while the medicine is injected is advisable and changes quickly reverse after the drug is stopped or the infusion rate is decreased.

The drug can be given intramuscularly but is exceedingly painful when given by this route. It can also be given intralesionally when treating cutaneous leishmaniasis (i.e., injected directly into the area of infected skin) and again, this is exceedingly painful and does not give results superior to intravenous administration.

Sodium stibogluconate can also cause a reduced appetite, metallic taste in mouth, nausea, vomiting, diarrhoea, headache, tiredness, joint pains, muscle aches, dizziness, and anaphylaxis.

Special Warning

Renal impairment: Dosage adjustments may be necessary

Innovators Monograph

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FAQ

What is Nizozole used for?

Nizozole is a medication used in the management of acute hypertension.

How safe is Nizozole?

Toxic if swallowed, inhaled or absorbed through the skin. Contact with acids liberates hydrogen cyanide, a very toxic, flammable gas or liquid. May cause eye and skin irritation.

How does Nizozole work?

Nizozole works by releasing nitric oxide. Like all other drugs in that class,Nizozole works by relaxing blood vessels. Once in the body, Nizozole is quickly broken down into nitric oxide, a powerful vasodilator.

What are the common side effects of Nizozole?

Common side effects of Nizozole are include:

  • excessive low blood pressure,
  • abdominal pain,
  • apprehension,
  • sweating,
  • dizziness,
  • headache,
  • muscle twitching,
  • nausea,
  • palpitations,
  • restlessness,
  • retching,
  • chest discomfort,
  • slow or fast heart rate,
  • rash,
  • flushing, or
  • irritation at the infusion site.

Is Nizozole safe during pregnancy?

Nizozole has been used to alter blood pressure in severe hypertensive disease of pregnancy; however, concern exists in regard to potential lethal complications from cyanide toxicity in both mother and fetus.

Is Nizozole safe during breastfeeding?

If use of Nizozole is unavoidable, the mother should refrain from breastfeeding.

Can I drink alcohol with Nizozole?

Do not eat, drink or smoke when using Nizozole.

How is Nizozole administered?

Nizozole is a potent vasodilator and is administered as an IV infusion with intensive monitoring in place.

How long can Nizozole be administered?

The usual dose of Nizozole rate is 0.5-10 mcg/kg/min, but infusion at the maximum dose rate should never last more than 10 minutes. If blood pressure has not been adequately controlled after 10 minutes of infusion at the maximum rate, administration of Nizozole should be terminated immediately.

When do I take Nizozole?

Nizozole injection is used for lowering of blood pressure immediately in adults and children with high blood pressure.

When should not I take Nizozole?

You should not use Nizozole if you are allergic to it.

What is the half life of Nizozole?

The half-life elimination of Nizozole in circulation is roughly 2 minutes.

What is the antidote for Nizozole?

Treatment of cyanide toxicity requires the cessation of Nizozole and, for severe toxicity, use of the cyanide antidote kit. Cyanide toxicity from Nizozole may be prevented by concomitant administration of Nizozole infusions.

What does Nizozole do to cyanide?

Nizozole acts as a sulfur donor to detoxify cyanide to thiocyanate by the enzyme rhodanese, whereas hydroxocobalamin binds cyanide and forms the nontoxic cyanocobalamin, which is renally excreted.

What does Nizozole do to the heart?

In general, it improves hemodynamic and clinical status by reducing systemic vascular resistance, left ventricular filling pressure, and increasing cardiac output.

Can I take overdose of Nizozole?

Overdosage of Nizozole can be manifested as excessive hypotension or cyanide toxicity or as thiocyanate toxicity.

What is the indication of Nizozole?

  • Nizozole is indicated for the immediate reduction of blood pressure of adult and pediatric patients in hypertensive crises. Concomitant longer-acting antihypertensive medication should be administered so that the duration of treatment with sodium nitroprusside can be minimized.
  • Nizozole is also indicated for producing controlled hypotension in order to reduce bleeding during surgery.
  • Nizozole is also indicated for the treatment of acute congestive heart failure.

What happen If I missed Nizozole?

If you miss a dose of Nizozole, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.


*** Taking medicines without doctor's advice can cause long-term problems.
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