Sulphaguanidine
Sulphaguanidine Uses, Dosage, Side Effects, Food Interaction and all others data.
Inositol Niacinate is a vasodilator and lipid-lowering agent. It improves circulation by releasing histamine, which causes the blood vessels to dilate and breaks up a protein needed for the clotting of blood. It also prevents the formation of lipids in the body, which helps to lower cholesterol and triglyceride levels.
Inositol nicotinate mediates a vasodilatory, lipid-lowering and fibrinolytic effect on the cardiovascular system. Like other niacins, inositol nicotinate is a lipid-regulating agent that reduces the levels of plasma triglycerides, atherogenic apolipoprotein B (apoB)-containing lipoproteins (VLDL, LDL and lipoprotein a) while increasing antiatherogenic apoA-I-containing HDL levels [A19560].
| Trade Name | Sulphaguanidine |
| Generic | Inositol Nicotinate |
| Inositol Nicotinate Other Names | hexanicotol, Inositol hexanicotinate, Inositol niacinate, Inositol nicotinate, mesoinositol hexanicotinate, myo-inositol hexanicotinate |
| Type | Tablet |
| Formula | C42H30N6O12 |
| Weight | Average: 810.732 Monoisotopic: 810.19217043 |
| Groups | Approved, Withdrawn |
| Therapeutic Class | Nicotinic acid group, Oral nutritional preparations |
| Manufacturer | |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Sulphaguanidine has a fairly broad range of therapeutic applications. The most well researched conditions include the hyperlipidemias, Raynaud's disease and intermittent claudication. Promising applications, which bear further investigation, include its use for stasis ulcers, dysmenorrhea, dermatitis herpetiformis, alcoholism, diabetes, cancer prevention and hypertension.
How Sulphaguanidine works
Inositol nicotinate and other niacins directly and noncompetitively inhibit microsomal enzyme diacylglycerol acyltransferase 2 (DGAT2) responsible for esterification of fatty acids to form triglycerides, resulting in decreased triglyceride synthesis and hepatic atherogenic lipoprotein secretion. Inhibitied triglyceride synthesis results in accelerated intracellular hepatic apo B degradation and the decreased secretion of VLDL and LDL particles . Niacin also inhibits hepatic expression of beta-chain adenosine triphosphate synthase which inhibits the removal or uptake of HDL–apo A-I. It is also suggested that niacin increases vascular endothelial cell redox state, resulting in the inhibition of oxidative stress and vascular inflammatory genes or key cytokines involved in atherosclerosis. It acts as a ligand on G-protein coupled receptor 109A (HCAR2/HM74A) and 109B (HCAR3/HM74) which mediates the anti-lipolytic and lipid-lowering effects of nicotinic acid. Niacin-mediated signalling of GPR109A expressed on adipocytes and G(i)-mediated decrease in cAMP levels result in decreased lipolysis, fatty acid mobilization, and triglyceride synthesis. The action of inositol nicotinate on GPR109A expressed on skin and macrophages to cause increased prostaglandin D2/E2 activity is thought to be less significant compared to other niacin molecules as it involves sustained release that leads to less flushing .
Dosage
Sulphaguanidine dosage
Recommended dosage for lipid-lowering and improving conditions related to peripheral vascular insufficiency ranges from 1500 mg to 4000 mg daily, in divided dosages of two to three times daily.
Side Effects
The most common side effects are headache, rash, paraesthesia, dizziness, nausea and vomiting, flushing, excessive fluid retention in the body tissues, postural hypotension, fainting
Toxicity
NOAEL is 4000mg. Inositol nicotinate can cause muscle pain, headache, redness of face, nausea, vomiting, edema and rash.
Precaution
Cautions should be exercised in patients with angina not well controlled by medical treatment and decreased blood supply through the vessels of the brain (cerebrovascular insufficiency).
Food Interaction
No interactions found.Volume of Distribution
Mean Vd following intravenous administration of 50mg/kg of inositol nicotinate in rats is 1051±250 mL/kg .
Elimination Route
Gastrointestinal absorption of inositol hexanicotinate varies widely, with an average of 70% of an orally ingested dose absorbed from stomach and upper small intestines into the bloodstream as intact form. The maximum serum levels of nicotinic acid is reached approximately 6-10 hours after oral ingestion. At low concentrations, the absorption of nicotinic acid and nicotinamide is mediated by sodium ion-dependent facilitated diffusion. At higher concentrations, passive diffusion predominates with doses of 3 to 4 g of niacin being almost completely absorbed .
Half Life
Mean elimination half life in healthy human adults is approximately one hour .
Clearance
Mean clearance rate following intravenous administration of 50mg/kg of inositol nicotinate in rats is 65.4±19 mL/min/kg .
Elimination Route
Unabsorbed inositol nicotinate is detected in feces.
Pregnancy & Breastfeeding use
Pregnancy: There is no information available about the safety of this medicine during pregnancy, therefore it is not recommended for use during pregnancy, unless considered essential by your doctor. Seek medical advice from your doctor.
Lactation: There is no information available regarding the safety of this medicine during breastfeeding
Contraindication
Inositol nicotinate is contraindicated to children, early stage of stroke & people who have recently had a heart attack. It should not be used if anyone is allergic to one or any of its ingredients
Acute Overdose
Both acute and chronic toxicities have been reported from the use of highdose niacin. Reactions to niacin range from acute symptoms of flushing, pruritis, and GI complaints to chronic symptoms of hepatotoxicity, hyperuricemia, and impaired glucose tolerance. On the other hand, no adverse effects have been reported from the use of inositol hexaniacinate in dosages as high as four grams daily
Storage Condition
Should be stored in cool and dry place
Innovators Monograph
You find simplified version here Sulphaguanidine
Sulphaguanidine contains Inositol Nicotinate see full prescribing information from innovator Sulphaguanidine Monograph, Sulphaguanidine MSDS, Sulphaguanidine FDA label
FAQ
What is Sulphaguanidine used for?
Sulphaguanidine is used for blood circulation problems, including a painful response to cold, especially in the fingers and toes. It is also used for high cholesterol, high blood pressure, and many other conditions, but there is no good scientific evidence to support these uses.Sulphaguanidine used to prevents a structural role in your body as a major component of cell membranes . It also influences the action of insulin, a hormone essential for blood sugar control. In addition, it affects chemical messengers in your brain.
How safe is Sulphaguanidine?
Stay on the safe side and avoid use. Allergies niacin, a chemical that is released when Sulphaguanidine breaks down in the body, might make allergies worse by releasing histamine.
How does Sulphaguanidine work?
Sulphaguanidine releases niacin, or vitamin B3, when it is processed by the body.Sulphaguanidine can widen blood vessels, lower blood levels of fats such as cholesterol, and break up a protein needed for the clotting of blood.
What are the common side effects of Sulphaguanidine?
Common side effects of Sulphaguanidine are include: stomach upset, headache, nausea, burping, and hiccups. It might also cause liver damage like other niacin products in some people.
Is Sulphaguanidine safe during pregnancy?
There is not enough reliable information about the safety of taking Sulphaguanidine if you are pregnant. Stay on the safe side and avoid use.
Is Sulphaguanidine safe during breastfeeding?
Sulphaguanidine is likely safe for pregnant and breast-feeding women when taken in the recommended amounts. The recommended amount of Sulphaguanidine for breastfeeding women is 30 mg per day for women under 18 years of age, and 35 mg for women over 18.
Can I drink alcohol with Sulphaguanidine?
Avoid alcohol, hot drinks, or spicy foods when it is time to take Sulphaguanidine.
How long does it take for Sulphaguanidine to work?
Sulphaguanidine take to work within 20 minutes of an oral dose and persists for about 20-60 minutes.
What is the best time to take Sulphaguanidine?
If you take more than one capsule, take one before Breakfast and one before Lunch or Dinner. If splitting the dosage doesn't work for you, then taking two capsules before food is also fine.
When is the best time to take Sulphaguanidine?
Sulphaguanidine should be taken with food. The extended-release form of niacin should be taken at bedtime.
When is the best time to take Sulphaguanidine?
Sulphaguanidine might also cause liver damage like other niacin products in some people.
Can I take Sulphaguanidine for long term?
Sulphaguanidine supplements are safe for long-term use. In most studies, inositol supplements were only taken for a year or less.
How much Sulphaguanidine can I take daily?
There is no recommended daily allowance for Sulphaguanidine. Most studies administer between 10 - 18 grams pre day of inositol to achieve desired results with minimal to no side effects.
Does Sulphaguanidine grow hair?
Sulphaguanidine is important for hair growth.
Is Sulphaguanidine good for my liver?
Sulphaguanidine have been shown to prevent abnormal or excessive liver accumulation of cholesterol and triglycerides in choline and myoinositol deficient rats.
Is Sulphaguanidine good for skin?
Sulphaguanidine was found to improve the clinical condition of skin by reducing hyperandrogenism in women with moderate acne, and is nominated as a useful adjunct therapy for women with both PCOS and acne , that is as part of a wider treatment plan.
Can Sulphaguanidine affect kidneys?
Sulphaguanidine a chemical that is released when Sulphaguanidine breaks down in the body, might accumulate in people with kidney disease and make their condition worse. Don't use Sulphaguanidine if you have kidney problems.
Can Sulphaguanidine causes low blood pressure?
Sulphaguanidine a chemical that is released when Sulphaguanidine breaks down in the body, can cause low blood pressure.
Who should not take Sulphaguanidine?
Sulphaguanidine is contraindicated in patients with gout, gallbladder disorders, allergies, bleeding disorders, gout, hypotension, angina, peptic ulcer with or without perforations, CAD and diabetes. Sulphaguanidine should not be prescribed to individuals who are allergic to synthetic form of niacin.
Can I overdose on Sulphaguanidine?
If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.
What should I do if I miss a dose?
Take a missed dose as soon as you think about it, with a meal.If it is close to the time for your next dose, skip the missed dose and go back to your normal time.Do not take 2 doses at the same time or extra doses.
