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Desvenlafaxine

Overview

Desvenlafaxine is a serotonin and norepinephrine reuptake inhibitor (SNRI) antidepressant. Desvenlafaxine is used to treat major depressive disorder. It is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class.

Chemical name of Desvenlafaxine is 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol. Its molecular formula is C16H25NO2 and molecular weight is 263.38.

Desvenlafaxine is a white to off-white, crystalline powder that is sparingly soluble in Dimethyl sulfoxide.

Clinical Applications

Desvenlafaxine is used to treat major depressive disorder in adults. For healthy women who have contraindications to estrogen, clinicians can use desvenlafaxine off-label to treat hot flashes during menopause.

Mode of Administration

Desvenlafaxine administration is via oral route and can be taken with or without food.

Pharmacological Effects

Desvenlafaxine works by increasing the levels of chemical messengers (serotonin and noradrenaline), natural substances in the brain that help maintain mental balance.

Dexmedetomidine Hydrochloride

Overview

Dexmedetomidine Hydrochloride is a central alpha-2-adrenergic agonist, an imidazole derivate with analgesic, anxiolytic and sedative activities.

Dexmedetomidine Hydrochloride is the S-enantiomer of Medetomidine Hydrochloride. Chemical name of Dexmedetomidine Hydrochloride is 1H-Imidazole, 4-[1-(2,3-dimethyl phenyl)ethyl]-, monohydrochloride, (S). Dexmedetomidine Hydrochloride has a molecular weight of 236.74 and the molecular formula is C13H16N2.HCl.

Dexmedetomidine Hydrochloride is a white or almost white powder that is freely soluble in water. Its melting range is 156-158°C.

Clinical Applications

Intensive Care Unit Sedation

Dexmedetomidine Hydrochloride is indicated for sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting.

Procedural Sedation

Dexmedetomidine Hydrochloride is indicated for sedation of non-intubated patients prior to and/or during surgical and other procedures.

Mode of Administration

Dexmedetomidine Hydrochloride is available in injectable form.

Pharmacological Effects

Dexmedetomidine produces sedation while maintaining a degree of arousability and may reduce the duration of mechanical ventilation and delirium among patients in the intensive care unit (ICU).

Digoxin

Overview

Digoxin is a cardiotonic drug. It is widely used in the treatment of various heart conditions, namely atrial fibrillation, atrial flutter and congestive heart failure that cannot be controlled by other medication.

Digoxin is extracted from the leaves of Digitalis lanata.

Digoxin is described chemically as 3β-[(O-2,6-dideoxy-β-D-ribo-hexopyranosyl-(1→4)-O-2,6-dideoxy-β-D-ribo-hexopyranosyl-(1→4)-2,6-dideoxy-β-D-ribo-hexopyranosyl)oxy]-12β,14-dihydroxy-5β-card-20(22)-enolide. Its molecular formula is C41H64O14, its molecular weight is 780.95.

Digoxin exists as white to almost white powder that melts with decomposition above 230°C. The drug substance is practically insoluble in Water, slightly soluble in Ethanol (96%) and soluble in a mixture of equal volumes of Methanol and Methylene dichloride.

Clinical Applications

Digoxin is used in the treatment of heart failure and in certain supraventricular arrhythmias, particularly atrial fibrillation and atrial flutter.

Mode of Administration

Digoxin is most often administered orally. It can also be given as a slow intravenous infusion in an emergency, although this is rarely necessary.

Pharmacological Effects

Digoxin increases the force of contraction of the heart and slows the resting heart rate. It also slows conduction through the atrioventricular node and works in this way to terminate or reduce the risk of recurrence of supraventricular tachycardia.

Forskolin

Overview

Forskolin (Coleonol) is a labdane diterpene produced by the plant Coleus forskohlii. Other names include pashanabhedi, Indian coleus, makandi, HL-362, maohouqiaoruihua. Forskolin is commonly used in laboratory research to increase levels of cyclic AMP by stimulation of adenylate cyclase.

Forskolin contains some unique functional elements, including the presence of a tetrahydropyran-derived heterocyclic ring. Forskolin is chemically described as (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-3-Ethenyl-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxododecahydro-1H-naphtho[2,1-b] pyran-5-yl acetate. Its molecular formula is C22H34O7, which corresponds to a molecular weight of 410.5.

Forskolin is a white to off-white powder. Its melting point is 228-232°C.

Clinical Applications

Forskolin is a herbal supplement which can be used as a natural remedy for treatment in cancer, obesity, glaucoma, allergies and asthma, heart failure, intestinal spasms, painful cramps during period (dysmenorrhea), irritable bowel syndrome, urinary tract infection, high blood pressure (hypertension), chest pain (angina), difficulty falling asleep (insomnia) and convulsions. Small clinical studies indicate obesity reduction potential as well as asthma prevention.

Mode of Administration

Forskolin is given by oral or inhalation route.

Pharmacological Effects

Forskolin activates the enzyme adenylyl cyclase and increases intracellular levels of cAMP. cAMP is an important second messenger necessary for the proper biological response of cells to hormones and other extracellular signals. It is required for cell communication in the hypothalamus/pituitary gland axis and for the feedback control of hormones via induction of corticotropin-releasing factor gene transcription. Cyclic AMP acts by activating cAMP-sensitive pathways such as protein kinase A and EPAC1.

Hydroxocobalamin Acetate

Overview

Hydroxocobalamin Acetate is a synthetic form of vitamin B12 that can be used as a dietary supplement to treat vitamin B12 deficiency. It is a physiological analogue of vitamin B12, where the CN group is replaced with OH. It is a Coordination Compound. Chemical name of Hydroxocobalamin Acetate is Coα-[α-(5,6-dimethylbenzimidazolyl)]-Coβ-hydroxocobamide acetate. Its molecular formula is C64H93CoN13O17P and molecular weight is 1406.0. Hydroxocobalamin Acetate is dark red, crystalline powder or dark red crystals that is soluble in Water. It has a melting point of about 271°C.

Clinical Applications

Hydroxocobalamin Acetate is an injectable form of vitamin B12 that has been used therapeutically to treat vitamin B12 deficiency. It is also used in cyanide poisoning, Leber's optic atrophy, and toxic amblyopia.

Mode of Administration

Hydroxocobalamin is given by injection into a muscle or vein.

Pharmacological Effects

Upon administration, Hydroxocobalamin mimics vitamin B12 and acts as an essential cofactor in various cellular reactions required for cell growth and replication, and hematopoiesis.

Hydroxocobalamin Chloride

Overview

Hydroxocobalamin Chloride is a synthetic form of vitamin B12 that can be used as a dietary supplement to treat vitamin B12 deficiency. It is a physiological analogue of vitamin B12, where the CN group is replaced with OH. It is a Coordination Compound.

Chemical name of Hydroxocobalamin Chloride is Cobinamide, dihydroxide, dihydrogen phosphate (ester), mono (inner salt), 3’-ester with 5,6-dimethyl-1-α-D-ribofuranosyl-1H-benzimidazole hydrochloride. Its molecular formula is C62H89CoN13O15P·HCl and molecular weight is 1382.82.

Hydroxocobalamin Chloride is dark red, crystalline powder or dark red crystals and is soluble in Water.

Clinical Applications

Hydroxocobalamin is used therapeutically to treat vitamin B12 deficiency. It is also used in cyanide poisoning, Leber's optic atrophy, and toxic amblyopia.

Mode of Administration

Hydroxocobalamin is given by injection into a muscle or vein.

Pharmacological Effects

Upon administration, Hydroxocobalamin mimics vitamin B12 and acts as an essential cofactor in various cellular reactions required for cell growth and replication, and hematopoiesis.

Hydroxocobalamin Sulphate

Overview

Hydroxocobalamin Sulphate is a synthetic form of vitamin B12 that can be used as a dietary supplement to treat vitamin B12 deficiency. It is a physiological analogue of vitamin B12, where the CN group is replaced with OH. It is a Coordination Compound.

Chemical name of Hydroxocobalamin Sulphate is Cobinamidedihydroxide dihydrogen phosphate (ester), mono (inner salt), 3'-ester with 5,6-dimethyl-1-α-D-ribofuranosyl-1H-benzimidazole Sulphate (salt). Its molecular formula is C62H89CoN13O17PS and molecular weight is 1410.42.

Hydroxocobalamin Sulphate is dark red, crystalline powder or dark red crystals and is soluble in Water.

Clinical Applications

Hydroxocobalamin is used therapeutically to treat vitamin B12 deficiency. It is also used in cyanide poisoning, Leber's optic atrophy, and toxic amblyopia.

Mode of Administration

Hydroxocobalamin is given by injection into a muscle or vein.

Pharmacological Effects

Upon administration, Hydroxocobalamin mimics vitamin B12 and acts as an essential cofactor in various cellular reactions required for cell growth and replication, and hematopoiesis.

Indacaterol Maleate

Overview

Indacaterol maleate is used for treatment of Chronic Obstructive Pulmonary Disease. It has a role as a beta-adrenergic agonist and a bronchodilator agent. The maleate salt is obtained by reaction of Indacaterol with one equivalent of Maleic acid.

The chemical name of Indacaterol maleate is (R)-5-[2-(5,6-Diethylindan-2-ylamino)-1- hydroxyethyl]-8-hydroxy-1H-quinolin-2-one maleate corresponding to the molecular formula C24H28N2O3.C4H4O4 and molecular weight of 508.56.

Indacaterol maleate appears as a white to slightly greyish or slightly yellowish powder that is freely soluble in N-Methyl pyrrolidone and practically insoluble in Ethyl acetate. Its melting point is 195-197°C (dec.)

Clinical Applications

Indacaterol maleate is used for the treatment of Chronic Obstructive Pulmonary Disease (COPD). It is delivered as an aerosol formulation through a dry powder inhaler.

Mode of Administration

Indacaterol inhalation comes as a powder-filled capsule to inhale by mouth using a special inhaler.

Pharmacological Effects

Indacaterol works by stimulating adrenergic beta-2 receptors in the smooth muscle of the airways. This causes relaxation of the muscle, thereby increasing the diameter of the airways, which become constricted in asthma and COPD. It is also long-acting due to its high affinity to the lipid raft domains in the airway membrane so it slowly dissociates from the receptors. Indacaterol also has a high intrinsic efficacy, so it is also very rapid acting.

Lanatoside C

Overview

Lanatoside C is an antiarrhythmic agent, naturally occurring compound extracted from Digitalis lanata. It is a cardiac glycoside, a type of drug that can be used in the treatment of congestive heart failure and cardiac arrhythmia (irregular heartbeat).

The substance is composed of four monosaccharides (glucose, 3-acetyldigitoxose and two digitoxoses) and an aglycon named digoxigenin. Chemical name of Lanatoside C is 3β,5β,12β)- 3-{[β-D- glucopyranosyl- (1→4)- 3-O-acetyl- 2,6-dideoxy- β-D-ribo- hexopyranosyl- (1→4)- 2,6-dideoxy- β-D- ribo- hexopyranosyl- (1→4)- 2,6-dideoxy- β-D- ribo- hexopyranosyl]oxy}- 12,14-dihydroxycard- 20(22)- enolide. Its molecular formula is C49H76O20 that corresponds to molecular weight of 985.12.

Lanatoside C appears as a colourless or white crystals or white crystalline powder. It is odourless. Its melting point is 246-248°C.

Clinical Applications

Main indications of Lanatoside C are rapid response atrial fibrilation and paroxysmal supraventricular tachycardia, two common types of arrhythmia.

Mode of Administration

Lanatoside C can be used orally or by the intravenous route.

Pharmacological Effects

Lanatoside exerts positive inotropic effect by increasing the concentration of intracellular Calcium, thereby increasing myocardial contraction.

Lysergol

Overview

Lysergol is an alkaloid of the ergoline family that occurs as a minor constituent in some species of fungi (most within Claviceps), and in the morning glory family of plants (Convolvulaceae), including the hallucinogenic seeds of Riveacorymbosa (ololiuhqui), Argyreia nervosa (Hawaiian baby woodrose) and Ipomoea hederacea. Lysergol is a starting material for the synthesis of the anti-Parkinson drug – Cabergoline, and an intermediate in the manufacture of ergoloid medicine -Nicergoline. Lysergol is chemically described as [(6aR,9R)-7-Methyl-4,6,6a,7,8,9-hexahydroindolo[4,3-fg]quinolin-9-yl]methanol. Its molecular formula is C16H18N2O, which corresponds to a molecular weight of 254.33. Lysergol is off-white to pale brown fine powder. Its melting point is >183°C (dec.)

Potential Applications

Lysergol has been used as hypotensive, psychotropic analgesic and uterus and intestine-stimulating drug.

Recently invented the novel bio-enhancing potential of Lysergol, which acts as bioavailability facilitator for antibiotics and helps in transferring the antibiotics across the membrane for better efficacy on the target site.

As a starting material for the synthesis of modern anti-Parkinson drug - Cabergoline.

As an intermediate in the manufacture of ergoloid medicine – Nicergoline.