Archives

Monoammonium Glycyrrhizinate (MAG)

Overview

Monoammonium glycyrrhizinate is an ammonium salt of glycyrrhizin, which is the major triterpenoid saponin of licorice root (Glycyrrhiza glabra). It has been widely used for the treatment of various inflammatory-based skin diseases. Therefore, its various delivery systems have been reported. It is also an agonist of the human sweet taste receptor, and is known to be a natural sweetener.

Chemical name of Monoammonium glycyrrhizinate is azanium;(2S,3S,4S,5R,6S)-6-[[(3S,4aR,6aR,6bS,8aS,11S,12aR,14aR,14bS)-11-carboxy-4,4,6a,6b,8a,11,14b-heptamethyl-14-oxo-2,3,4a,5,6,7,8,9,10,12,12a,14a-dodecahydro-1H-picen-3-yl]oxy]-5-[(2R,3R,4S,5S,6S)-6-carboxy-3,4,5-trihydroxyoxan-2-yl]oxy-3,4-dihydroxyoxane-2-carboxylate. Its molecular formula is C42H65NO16 and molecular weight is 839.96.

Monoammonium glycyrrhizinate is a white to yellowish-white powder that is slightly soluble in Water, very slightly soluble in anhydrous Ethanol and practically insoluble in Acetone. Its Melting point is about 209°C.

Clinical Applications

Monoammonium glycyrrhizinate is used topically for allergic or infectious skin inflammation and orally for its aldosterone effects in electrolyte regulation.

Mode of Administration

Topical and oral.

Brivaracetam

Overview

Brivaracetam is a racetam derivative with anticonvulsant (antiepileptic) properties. Chemical name of Brivaracetam is (2S)-2-[(4R)-2-oxo-4-propylpyrrolidin-1-yl] butanamide. Its molecular formula is C11H20N2O2 and molecular weight is 212.29.

Brivaracetam is a white to off-white coloured powder that is very soluble in Dimethyl formamide and freely soluble in Methanol. Its melting point is 72 to 77°C.

Clinical Applications

Brivaracetam is an anticonvulsant used for the treatment of partial-onset seizures.

Mode of Administration

Brivaracetam is administered by oral or intravenous routes.

Pharmacological Effects

Brivaracetam functions by binding to synaptic vesicle glycoprotein 2A (SV2A) in the brain with high affinity. SV2A is known to play a role in epileptogenesis through modulation of synaptic GABA release. It is thought that Brivaracetam exerts its anti-epileptogenic effects through its binding to SV2A. Brivaracetam is also known to inhibit Na+ channels which may also contribute to its anti-epileptogenic action.

Pramipexole Dihydrochloride Monohydrate

Overview

Pramipexole dihydrochloride is the hydrochloride salt of Pramipexole, a benzothiazole derivative. Pramipexole dihydrochloride monohydrate is a medication used to treat Parkinson's disease (PD) and restless legs syndrome (RLS). It is a dopamine agonist of the non-ergoline class.

Pramipexole dihydrochloride monohydrate is described chemically as (S)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole dihydrochloride monohydrate. Its molecular formula is C10H17N3S.2HCl.H2O, and its molecular weight is 302.26.

Pramipexole dihydrochloride monohydrate is a white to almost white, crystalline powder that is freely soluble in Water, soluble in Methanol, slightly soluble in Alcohol, practically insoluble in Methylene dichloride. Melting range is 296°C to 301°C, with decomposition.

Clinical Applications

Pramipexole dihydrochloride monohydrate is indicated for the symptomatic treatment of Parkinson’s disease. It is also indicated for symptomatic treatment of moderate to severe primary Restless legs syndrome.

Mode of Administration

Pramipexole dihydrochloride monohydrate is taken by mouth.

Pharmacological Effects

Parkinson's Disease

Through the stimulation of dopamine receptors, Pramipexole is thought to relieve the symptoms of Parkinson's disease. The motor symptoms of Parkinson's disease occur partly due to a reduction of dopamine in the substantia nigra of the brain. Dopamine is an essential neurotransmitter that has major effects on motor movements in humans.

Restless Legs Syndrome

Pramipexole likely restores balance to the dopaminergic system, controlling the symptoms of this condition. Restless legs syndrome is thought to occur, in part, through dysfunction of the dopaminergic system, resulting in unpleasant lower extremity symptoms.

10-DAB III

Overview

10-Deacetylbaccatin III (10-DAB III) is used as an API intermediate in the preparation of the anti-cancer drugs - Paclitaxel, Docetaxel and Cabazitaxel.

10-DAB III is extracted from the leaves of Yew tree (Genus –Taxus).

10-DAB III is a tetracyclic diterpenoid and a secondary alpha-hydroxy ketone. It is described chemically as (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-(Acetyloxy)-12-(benzoyloxy)-1,2a,3,4,4a,6,9,10,11,12,12a,12b-dodecahydro-4,6,9,11-tetrahydroxy-4a,8,13,13-tetramethyl-7,11-methano-5H-cyclodeca(3,4)benz(1,2-b)oxet-5-one. Its molecular formula is C29H36O10, its molecular weight is 544.59.

10-DAB III exists as white to off-white powder having melting point between 229-239°C. The drug intermediate is freely soluble in Dimethyl formamide and Dimethyl sulphoxide, soluble in Methanol, slightly soluble in Ethanol (95%) and Acetone, insoluble in Water, Ethyl acetate, Chloroform, Dichloromethane, Acetonitrile, aq. HCl and aq. NaOH solutions.

Adenosylcobalamin / Cobamamide

Overview

Adenosylcobalamin, also known as coenzyme B12, cobamamide and dibencozide is one of the biologically active forms of vitamin B12. It is used to treat vitamin B12 deficiency due to dietary deficiency or malabsorption.

Adenosylcobalamin is described chemically as Coα-[α-(5,6-dimethylbenzimidazolyl)]-Coβ-(5'-deoxy-5'-adenosyl)cobamide. Its molecular formula is C72H100CoN18O17P, its molecular weight is 1579.

Adenosylcobalamin exists as dark red crystals or a powder that is sparingly soluble in Water and insoluble in Ethanol.

Clinical Applications

Peripheral Neuropathy - To relieve the symptoms of nerve damage in the feet and hands.
Vitamin B12 deficiency- To treat dietary deficiency or malabsorption.
Megaloblastic Anaemia - To treat anaemia due to deficiency of Vitamin B12.

Mode of Administration

Adenosylcobalamin should be taken orally.
It is usually available as a combination with other supplements.

Pharmacological Effects

In humans, Adenosylcobalamin plays an essential role in the production of blood and the maintenance of normal cerebral and nervous function in the human body. It is involved in the synthesis of thymidylate, a substance necessary for DNA synthesis.

Aescin

Overview

Aescin or Escin is a mixture of saponins with anti-inflammatory, vasoconstrictor and vasoprotective effects found in Aesculus hippocastanum/indica (the horse chestnut). Aescin is the main active compound in horse chestnut and is responsible for most of its medicinal properties such as venotonic effect, treatment of cellulitism, vascular disorder, cosmetics for prevention, anti-inflammatory and free radical scavenging properties.

Aescin is described chemically as 6-[[9-acetyloxy-8-hydroxy-4,8a-bis(hydroxymethyl)-4,6a,6b,11,11,14b-hexamethyl-10-(2-methylbut-2-enoyloxy)-1,2,3,4a,5,6,7,8,9,10,12,12a,14, 14a-tetradecahydropicen-3-yl]oxy]-4-hydroxy-3,5-bis[[3,4,5-trihydroxy-6-(hydroxymethyl) oxan-2-yl]oxy]oxane-2-carboxylic acid. Its molecular formula is C55H86O24, its molecular weight is 1131.26.

Aescin exists as a white or whitish powder that is soluble in Methanol and sparingly soluble in Water. Its melting point is about 225°C.

Clinical Applications

Primary indication is chronic venous insufficiency. Further, Aescin is a saponin complex and its main effect is anti-inflammatory.

Mode of Administration

Aescin is taken orally for venous insufficiency and is available in tablet form. Oral tinctures and topical gels are also available.

Pharmacological Effects

Aescin appears to produce effects through a wide range of mechanisms. It induces endothelial nitric oxide synthesis by making endothelial cells more permeable to calcium ions, and also induces release of prostaglandin. Other possible mechanisms include serotonin antagonism and histamine antagonism and reduced catabolism of tissue mucopolysaccharides.

Apixaban

Overview

Apixaban is an anticoagulant used for the prophylaxis of stroke and systemic embolism in nonvalvular atrial fibrillation, and deep vein thrombosis (DVT) leading to pulmonary embolism (PE), including in patients after a hip or knee replacement surgery.

Apixaban is chemically described as 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1 H-pyrazolo[3,4- c]pyridine-3- carboxamide. Its molecular formula is C25H25N5O4, which corresponds to a molecular weight of 459.5.

Apixaban exists as a white to pale yellow powder that is sparingly soluble in N, N-Dimethylformamide and practically insoluble in Water. Its melting point is about 238°C.

Clinical Applications

To reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation
For the prophylaxis of deep vein thrombosis (DVT), which may lead to pulmonary embolism (PE) in patients who have undergone hip or knee replacement surgery.
For the treatment of DVT and PE and for the reduction in the risk of recurrent DVT and PE therapy.

Mode of Administration

Apixaban is taken orally in tablet form.

Pharmacological Effects

Apixaban is a selective inhibitor of FXa. It does not require antithrombin III for antithrombotic activity. Apixaban inhibits free and clot-bound FXa, and prothrombinase activity. Apixaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, Apixaban decreases thrombin generation and thrombus development.

Artemether

Overview

Artemether is an antimalarial agent used to treat acute uncomplicated malaria. Artemether is an artemisinin derivative, in which the lactone has been converted to the corresponding lactol methyl ether. Artemether is chemically described as (3R,5aS,6R,8aS,9R,10S,12R,12aR)-10-methoxy-3,6,9-trimethyldecahydro-3,12-epoxypyrano [4,3-j]-1,2-benzodioxepine. Its molecular formula is C16H26O5, which corresponds to a molecular weight of 298.37.

Artemether appears as white crystals or a white, crystalline powder that is practically insoluble in Water, very soluble in Dichloromethane and Acetone, freely soluble in Ethyl acetate and dehydrated Ethanol. Its melting range is 86 to 90°C.

Clinical Applications

For uncomplicated malaria caused by P. falciparum (and chloroquine-resistant P. falciparum) or chloroquine-resistant P. vivax parasites.
Artemether can also be used to treat severe malaria.
For enhanced efficacy, it is given in combination with lumefantrine. This combination therapy exerts its effects against Plasmodium spp. erythrocytic stages.

Mode of Administration

Artemether is given by injection in a muscle. It is also available by mouth in combination with lumefantrine.

Pharmacological Effects

Artemether interacts with ferriprotoporphyrin IX (heme) or ferrous ions in the acidic parasite food vacuole and generates cytotoxic radical species. The accepted mode of action of the peroxide-containing drug involves its interaction with heme (byproduct of haemoglobin degradation), derived from proteolysis of haemoglobin. This interaction results in the formation of toxic oxygen and carbon-centred radicals.

Cabergoline

Overview

Cabergoline is a dopaminergic medication used in the treatment of high prolactin levels, prolactinomas, Parkinson's disease etc.

The chemical name for Cabergoline is 1-[(6-Allylergolin-8β-yl)-carbonyl]-1-[3-(dimethylamino) propyl]-3-ethylurea. Its molecular formula is C26H37N5O2 and its molecular weight is 451.60. Cabergoline is a white or almost white powder that is freely soluble in Alcohol (96%), slightly soluble in 0.1M Hydrochloric acid, very slightly soluble in Hexane, practically insoluble in Water. Its melting point is 97.5 to 100.5°C.

Clinical Applications

For the treatment of hyperprolactinemic disorders, either idiopathic or due to prolactinoma (prolactin-secreting adenomas). May also be used to manage symptoms of Parkinsonian Syndrome as monotherapy during initial symptomatic management or as an adjunct to levodopa therapy during advanced stages of disease.

Mode of Administration

Cabergoline is given orally as a tablet. It is usually taken with or without food two times a week.

Pharmacological Effects

Cabergoline is an ergot medication and works by blocking the release of prolactin from the pituitary gland. The secretion of prolactin by the anterior pituitary is mainly under hypothalamic inhibitory control, likely exerted through release of dopamine by tuberoinfundibular neurons. Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D receptors. Results of in vitro studies demonstrate that Cabergoline exerts a direct inhibitory effect on the secretion of prolactin.

Deslanoside

Overview

Deslanoside is a cardiac glycoside, a type of drug that can be used in the treatment of congestive heart failure and cardiac arrhythmia (irregular heartbeat). It is found in the leaves of Digitalis lanata, the Woolly Foxglove.

This compound belongs to the class of organic compounds known as cardenolide glycosides and derivatives. These are compounds containing a carbohydrate glycosidically bound to the cardenolide moiety. Deslanoside is chemically described as (3β,5β,12β)-3-[(O-β-D-gluco pyranosyl-(1→4)-O-2,6-dideoxy-β-D-ribo-hexopyranosyl-(1→4)-O-2,6-dideoxy-β-D-ribo-hexo pyranosyl-(1→4)-2,6-dideoxy-β-D-ribo hexopyranosyl)oxy]-12,14-dihydroxycard-20(22)-enolide. Its molecular formula is C47H74O19 and molecular weight is 943.09.

Deslanoside exists as a white crystalline powder that is slightly soluble in Methanol, very slightly soluble in Ethanol, practically insoluble in Water and in Chloroform. Its specific optical rotation is +7° to +9°.

Clinical Applications

For the treatment and management of congestive cardiac insufficiency, arrhythmias and heart failure.

Mode of Administration

Deslanoside is available in injectable form.

Pharmacological Effects

Deslanoside inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular Sodium and Calcium concentrations. Increased intracellular concentrations of Calcium may promote activation of contractile proteins (e.g., actin, myosin). Deslanoside also acts on the electrical activity of the heart, increasing the slope of phase 4 depolarization, shortening the action potential duration, and decreasing the maximal diastolic potential.