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Methylcobalamin

Overview

Methylcobalamin (Mecobalamin, MeCbl, or MeB12) is a cobalamin, a form of vitamin B12. It differs from Cyanocobalamin in that the cyano group at the cobalt is replaced with a methyl group. From the perspective of coordination chemistry, Methylcobalamin is notable as a rare example of a compound that contains metal–alkyl bonds.

Chemical name of Methylcobalamin is Coα-[α-(5,6-dimethyl-1H-benzimidazol-1-yl)]-Coβ-methylcobamide. Its molecular formula is C63H91CoN13O14P and its molecular weight is 1344.40.

Methylcobalamin appears as dark red crystals or crystalline powder that is sparingly soluble in Water, slightly soluble in Ethanol (99.5%) and practically insoluble in Acetonitrile. Its melting point is 232 to 235°C.

Clinical Applications

Methylcobalamin is used to treat vitamin B12 deficiency. Vitamin B12 is important for the brain and nerves and for the production of red blood cells.

Methylcobalamin is sometimes used in people with pernicious anaemia, diabetes, and other conditions.

Mode of Administration

Methylcobalamin can be administered via intranasal, oral and parenteral routes.

Pharmacological Effects

Methylcobalamin is an active form of vitamin B12 that helps in synthesis of methionine and S-adenosylmethionine. It is required for integrity of myelin, neuronal function, proper red blood cell formation and DNA synthesis. It is a beneficial drug to most of the common disorders like cardiovascular disorders, diabetes, anemia, hyperhomocysteinemia and degenerative disorders. Methylcobalamin helps in the synthesis of neuronal lipids, regeneration of axonal nerves and has neuroprotective activity, which promote neurons to function in proper way and thus improves Alzheimer’s disease, Parkinsonism, Dementia and neuropathic syndromes. It is an approved treatment for peripheral neuropathy.

Mirtazapine

Overview

Mirtazapine is a tetracyclic antidepressant used in the treatment of major depression and is used off-label as a drug for insomnia and to increase appetite.

Mirtazapine has a tetracyclic chemical structure and belongs to the piperazino-azepine group of compounds. It is chemically described as (±)-2-Methyl-1,2,3,4,10,14b-hexahydropyrazino[2,1-a]pyrido[2,3-c][2]benzazepine. Its molecular formula is C17H19N3 and molecular weight is 265.36.

Mirtazapine is a white to creamy white crystalline powder which is slightly soluble in Water, soluble in Methanol and Chloroform. Its melting point is 114 to 116°C.

Clinical Applications

Mirtazapine is indicated for the treatment of major depressive disorder and its associated symptoms.

Mirtazapine has been used off-label for a variety of conditions including panic disorder, generalized anxiety disorder, dysthymia, tension headaches, hot flushes, Post-Traumatic Stress Disorder (PTSD), sleep disorders, substance abuse disorders and sexual disorders, among others.

Mode of Administration

Mirtazapine is taken by mouth (tablets).

Pharmacological Effects

The mechanism of action of Mirtazapine may be explained by its effects on central adrenergic and serotonergic activity. This drug exhibits a fast onset of action, a high level of response, a manageable side-effect profile and dual noradrenergic and serotonergic effects that are unique from the effects of other antidepressants.

Nalbuphine Hydrochloride

Overview

Nalbuphine Hydrochloride is a synthetic opioid agonist-antagonist analgesic of the phenanthrene series. Chemically Nalbuphine Hydrochloride is 17-(Cyclobutylmethyl)-4,5α-epoxymorphinan-3,6α,14-triol hydrochloride. Molecular formula of Nalbuphine Hydrochloride is C21H28ClNO4 and molecular weight is 393.91.

Nalbuphine Hydrochloride appears as a white to almost white powder that is soluble in Water and Ethanol, insoluble in Chloroform and Ether. Its melting point is about 230°C.

Clinical Applications

Nalbuphine Hydrochloride is indicated for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. Nalbuphine Hydrochloride can also be used as a supplement to balanced anaesthesia, for preoperative and postoperative analgesia and for obstetrical analgesia during labour and delivery.

Mode of Administration

Nalbuphine Hydrochloride is administered in injection form, as a solution (liquid) to inject subcutaneously (under the skin), intravenously (into a vein), or intramuscularly (into a muscle).

Pharmacological Effects

Nalbuphine Hydrochloride binds to kappa-, mu- and delta-opioid receptors but not to sigma-opioid receptors. This Opioid analgesic exerts its analgesic actions primarily through kappa-opioid-receptor agonism and partially through mu-opioid receptor agonism.

Naloxone Hydrochloride

Overview

Naloxone Hydrochloride is an opioid antagonist. It is chemically described as 4,5α-Epoxy-3,14-dihydroxy-17-(prop-2-enyl)morphinan-6-one hydrochloride dihydrate. Molecular formula of Naloxone Hydrochloride is C19H22ClNO4.2H2O and molecular weight is 399.9.

Naloxone Hydrochloride dihydrate appears as a white to almost white, crystalline powder, and is freely soluble in Water, soluble in Ethanol (96%), practically insoluble in Toluene. Its melting range is 138-140°C.

Clinical Applications

Naloxone Hydrochloride is an opioid antagonist medication used to block or reverse the effects of opioid drugs, particularly within the setting of drug overdoses which are rapidly becoming a leading cause of death worldwide.

Mode of Administration

Naloxone Hydrochloride is currently available by intramuscular (IM) or subcutaneous (SubQ) injection, nasal spray, or intravenous (IV) infusion.

Pharmacological Effects

Naloxone reverses the effects of opioid analgesics by binding to the opioid receptors in the CNS, and inhibiting the typical actions of opioid analgesics, including analgesia, euphoria, sedation, respiratory depression, miosis, bradycardia, and physical dependence. Naloxone binds to mu-opioid receptors with a high affinity, and a lesser degree to kappa- and gamma-opioid receptors in the CNS.

Naltrexone Hydrochloride

Overview

Naltrexone Hydrochloride is a medication primarily used to manage alcohol use or opioid use disorder by reducing cravings and feelings of euphoria associated with substance use disorder. Its chemical name is 17-(Cyclopropylmethyl)-4,5-α-epoxy-3,14-dihydroxy-morphinan-6-one hydrochloride. Its molecular formula is C20H24ClNO4 and molecular weight is 377.9.

Naltrexone Hydrochloride is a white to almost white powder that is freely soluble in Water, slightly soluble in Ethanol (96%), practically insoluble in Methylene chloride. Its melting point is 231-233°C.

Clinical Applications

Naltrexone Hydrochloride is indicated in the treatment of alcohol dependence and for the blockade of the effects of exogenously administered opioids.

Mode of Administration

Naltrexone Hydrochloride is taken by mouth or by injection into a muscle.

Pharmacological Effects

Naltrexone and its metabolite 6-beta-naltrexol reverse the effects of opioids by binding to various opioid receptors in the central nervous system (CNS), including the mu-, kappa- and gamma-opioid receptors; opioid effects of analgesia, euphoria, sedation, respiratory depression, miosis, bradycardia, and physical dependence are inhibited.

Neostigmine Methylsulfate

Overview

Neostigmine Methylsulfate is a prescription medicine used to treat the symptoms of Myasthenia gravis, reversal of non-depolarizing neuromuscular blockade and post-operative distention or urinary retention. Neostigmine Methylsulfate belongs to a class of drugs called Acetylcholinesterase Inhibitors, Peripheral.

Neostigmine Methylsulfate is chemically described as Benzenaminium,3-[[(Dimethylamino) carbonyl]oxy]-N, N, N-trimethyl-, methyl sulfate. Its molecular formula is C13H22N2O6S and molecular weight is 334.39.

Neostigmine Methylsulfate is a white or almost white crystalline powder that is very soluble in Water and freely soluble in Ethanol (96%). Its melting range is 144-149°C.

Clinical Applications

A cholinesterase inhibitor used in the treatment of Myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier.

Mode of Administration

Neostigmine can be given as an intramuscular (IM), intravenous (IV) or subcutaneous (SC) injection.

Pharmacological Effects

Neostigmine Methylsulfate is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. The drug inhibits acetylcholinesterase which is responsible for the degradation of acetylcholine. So, with acetylcholinesterase inhibited, more acetylcholine is present. By interfering with the breakdown of acetylcholine, Neostigmine indirectly stimulates both nicotinic and muscarinic receptors which are involved in muscle contraction.

Nepafenac

Overview

Nepafenac is an ophthalmic NSAID used for the symptomatic treatment of pain and inflammation associated with cataract surgery. Nepafenac is a prodrug of Amfenac, an inhibitor of COX-1 and COX-2 activity.

Chemical name of Nepafenac is 2-amino-3-benzoyl benzene acetamide. Its molecular formula is C15H14N2O2 and molecular weight is 254.29.

Nepafenac is a yellow crystalline powder that is soluble in Dimethyl sulfoxide, slightly soluble in Acetone, Methanol and Chloroform, practically insoluble in Water. Its melting point is 178-180°C.

Clinical Applications

Nepafenac is indicated for use in the treatment of pain and inflammation following cataract surgery.

Mode of Administration

Nepafenac is administered as Topical eye drops.

Pharmacological Effects

After topical ocular dosing, Nepafenac penetrates the cornea and is converted by ocular tissue hydrolases to Amfenac, a non-steroidal anti-inflammatory drug. Amfenac is thought to inhibit the action of prostaglandin H synthase (cyclooxygenase), an enzyme required for prostaglandin production.