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Showing posts from February, 2023

AZELASTINE used, Side dose, pharmacodynamic & mechanism of action......

 AZELASTINE BRAND NAME:- AZEP NASAL SPRAY 0.14mg   AZELASTINE is a second generation antihistamine drug .This is newer H1 blocker has good Topical activity; in addition it inhibits histamine realease and inflammatory reaction triggered by LTs and PAF. After intranasal application it has been shown to down regulate intracellular adhesion molecule -1 (ICAM-1) expression on nasal mucosa. Its t½ is 24hr,but action lasts longer due to active metabolite . Its metabolism is inhibited by CYP 3A4 inhibitors. Given by nasal spray for seasonal and perennial allergic rhinitis it provides quick symptomatic relief lasting 12hr.  PHARMACODYNAMIC:- Azelastine has a triple mode of action: Anti-histamine effect,Mast-cell stabilizing effect an Anti-inflammatory effect.  PHARMACOKINETICS:- The systemic bioavailability of azelastine is approximately 40% when administered intranasally.[3] Maximum plasma concentrations (Cmax) are observed within 2–3 hours.[3] The elimination half life, ste...

AZELAIC ACID : used, Side effects, dose, pharmacodynamic & mechanism of action....

 AZELAIC ACID 

AZIDOTHYMIDINE (AZT) / ZIDOVUDINE

 AZIDOTHYMIDINE (AZT) / ZIDOVUDINE  BRAND NAME:- RETROVIR, ZIDOVIR 100mg cap,50mg/5ml syr ,VIRO-Z , ZIDOMAX , ZYDOWN 100 mg cap, 300 mg tab. AZT / ZIDOVUDINE is a thymidine analogue,the prototype NRTI. After phosphorylation in the host cell- zidovudine triphosphate selectively inhibits viral reverse transcriptase in preference to cellular DNA polymerase. PHARMACOKINETICS:-  The oral absorption of AZT is rapid ,but bioavailability is ~ 65% . It is quickly cleared by hepatic glucuronidation (t½ 1 hr) ; 15-20% of the unchanged drug along with the metabolite is excerted in urine. Plasma proteins  binding is 30% and CSF level ~ 50% of that in plasma. It crosses placenta and is found in milk. PHARMACODYNAMIC:- Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Zidovudine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcr...

AZTREONAM

 AZTREONAM BRAND NAME:- AZENAM ,TREZAM 0.5,1.0,2.0 g/ vial inj . AZTREONAM is a novel Beta- lactam antibiotic in which the other ring is missing (hence monobactam ) , but acts by binding to specific PBPs. It inhibits gram- negative enteric bacilli and H.influenzae . PHARMACOLOGY:-  it is a novel Beta-lactam antibiotic in which the other ring is missing ( hence monobactam), but acts by binding to specific PBPs . It inhibits gram-negative enteric bacilli and H. Influenzae at very low concentrations and pseudomonas at moderate concentration,but does not inhibits gram - positive cocci or faecal anaerobes. Thus ,it is a Beta - lactam antibiotic with a spectrum resembling aminoglycosides,and is resistant to gram - negative Beta - lactamases . The main indications of Aztreonam are hospital acquired infection originating from urinary, biliary, Gastrointestinal and female genital tracts .  MECHANISM OF ACTION:- Aztreonam is similar in action to penicillin. The bactericidal action ...

ATOVAQUONE

 ATOVAQUONE BRAND NAME:- MEPRON  ATOVAQUONE is an antimicrobial indicated for the prevention and treatment of Pneumocystis jirovecii pneumonia (PCP) and for the prevention and treatment of Plasmodium falciparum malaria.  PHARMACOLOGY & MECHANISM OF ACTION:- This synthetic naphthoquinone is a rapidly acting erythrocytic schizontocide as well as active against preerythrocytic stage of P.falciparum and other plasmodia . Pneumocystis jiroveci and Toxoplasma gondii are also susceptible to atovaquone . It collapses plasmodial mitochondrial membrane and interferes with ATP production. Proguanil potentiates its antimalarial action and prevent emergence of resistance.  Atovaquone is a competitive inhibitor of ubiquinol, specifically inhibiting the mitochondrial electron transport chain at the bc1 complex. Inhibition of bc1 activity results in a loss of mitochondrial function. Several metabolic enzymes are linked to the mitochondrial electron transport chain via ubiquinone...

ATOSIBAN ; Used, side effects, Dose, Pharmacodynamic & mechanism of action

 ATOSIBAN 

ATOMOXETINE

 ATOMOXETINE BRAND NAME:- ATTENTROL 10,18,25,40mg caps AXEPTA 18,25mg caps . ATOMOXETINE is unrelated to Tricyclic antidepressant, but is a selective NA reuptake inhibitor . It is approved only for treatment of attention deficit hyperactivity disorder (ADHD).  PHARMACOLOGICAL & MECHANISM OF ACTION:- This is a selective NA reuptake inhibitor, unrelated to Amphetamine as well as to imipramine, which does not enhance DA release in the brain,and is neither a CNS stimulant nor an antidepressant. However,it has been found to improve attention span and behaviour in ADHD . It is indicated in children > 6 years and in adults with concentration and attention problems.   ATOMOXETINE is absorbed orally, hydroxylated by CYP2D6 and excreted in urine, mainly as glucuronide. While majority of individuals are extensive metabolizers (EM) ,few are poor Metabolizers (PM) due to polymorphism of CYP2D4 inhibitors of CYP2D6 like fluoxetine ,paroxetine, quinidine increase concentration an...

ASTEMIZOLE

 ASTEMIZOLE BRAND NAME:- Hismanal  ,Acipax, Alestol , Astem  ASTEMIZOLE are the earliest second generation H1 antihistamine drug. It treats allergy symptoms such as itching, swelling, and rashes by blocking the effects of a chemical messenger (histamine) in the body.  It has anticholinergic and antipruritic effects. PHARMACODYNAMIC:- Astemizole is a second generation H1-receptor antagonist. It has anticholinergic and antipruritic effects.It does not significantly cross the blood brain barrier and therefore does not cause drowsiness or CNS depression at normal doses. Several studies  have shown high permeability and high binding to protein folds associated with Alzheimer's. MECHANISM OF ACTION:-  Astemizole competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of astemizole to H1-receptors suppresses the formation of edema, flare, and pruritus resulting from histam...

ARTEROLANE - PIPERAQUINE

 ARTEROLANE+ PIPERAQUINE BRAND NAME:- Synriam ( arterolane malate 150mg + piperaquine 750mg )  ARTEROLANE MALEATE+PIPERAQUINE PHOSPHATE together treats malaria. They work by increasing the levels of heme in the blood, a substance toxic to the malarial parasite. This kills the parasite and stops the infection from spreading.        ARTEROLANE - PIPERAQUINE FDC has undergone multicentric clinical trials in India 🇮🇳, Bangladesh and Thailand. In uncomplicated falciparum malaria 🦟 this ACT has produced ≥ 95% cure rates with a fever and parasitaemia  clearance time 24-28 hours. In a comparative trail its efficacy and tolerability has been found equivalent to artemether - LUMEFANTRINE.  Thus arterolane - piperaquine appears to be an effective and well tolerated alternative ACT.    USED:- treatment of malaria 🦟. SIDE EFFECTS:-  are generally mild headache, postural dizziness, vomiting, abdominal pain and Diarrhoea. DOSE:- 1 CAP. OD for ...

ARTEROLANE MALEATE

 ARTEROLANE MALEATE  BRAND NAME:- no specific brand in single composition. ARTEROLANE, also known as OZ277 or RBx 11160, is a substance that was tested for antimalarial activity. Its molecular structure is uncommon for pharmacological compounds in that it has both an ozonide (trioxolane) group and an adamantane substituent.        MECHANISM & PHARMACOLOGICAL ACTION:-    ARTEROLANE acts rapidly at all stages of asexual schizogony  of malarial parasite including multidrug resistant P.f.,but has no effect on the hepatic stages. It accumulates in the food vacuole of the parasite,and thus differs from artemisinins which do not accumulates at this site. It also has moderate gametocidal activity similar to that of artemether - LUMEFANTRINE .  Arterolane are well absorbed orally, and absorption is unaffected by food. Peak plasma arterolane concentration is reached 3-5 hours and it has a large volume of distribution . The major metabolic path...

Know details about ARTEMISININ drug ?

 ARTEMISININ  BRAND NAME:- no specific brand available. ARTEMISININ is the active principal of the plant artemisia annua used in Chinese traditional medicine as ' Quinghaosu '  . It is a sesquiterpine lactones endoperoxide active against P. Falciparum resistant to all other antimalarial drugs as well as sensitive strains and other malarial species. MECHANISM OF ACTION:-  Of artemisinin is not definitely known. The endoperoxide brige in its molecules appears to interact with haeme in the parasite. Ferrous iron- mediated clevage of the brige release a highly reactive free radicals species that binds to membrane proteins, causes lipid peroxidation , damages endoplasmic reticulum ,and ultimately result in lysis of the parasite. Another line of evidence has shown that the artemisinin free radicals specifically inhibits a plasmodial sarcoplasma - endoplasmic calcium ATPase labelled 'PF ATP6'. Pharmacodynamic:-  🚫 Not available. Pharmacokinetics:- poor pharmacokinetic...

Know details learn about ARTEETHER drug ?

 ARTEETHER  BRAND NAME:- Artiz,Asth, Erod M etc. ARTEETHER is used for chloroquine resistant malaria, falciparum malaria and other cerebral malaria cases. It kills malarial parasites by interacting with heme.Arteether is an effective anti-malarial medicine . Arteether (i.m.) is slower acting than artesunate (i.v.) ,and appears to be less efficacious. It is used only in india. An injectable compound Arteether (i.m or i.v.) was produced in India in the 1990s. Pharmacodynamic:- In the body, artemether is metabolized into the active metabolite metabolite dihydroartemisinin. The drug works against the erythrocytic stages of P. falciparum by inhibiting nucleic acid and protein synthesis. Artemether is administered in combination with lumefantrine for improved efficacy. Artemether has a rapid onset of action and is rapidly cleared from the body. It is thought that artemether provides rapid symptomatic relief by reducing the number of malarial parasites. Lumefantrine has a much longer...

ARSENIC TRIOXIDE

 ARSENIC TRIOXIDE BRAND NAME:- Trisenox injection, ARSENIC TRIOXIDE has been a traditional poison for ages,and  is a chemotherapeutic agent used in the treatment of refractory or relapsed acute promyelocytic leukemia in patients with prior retinoid and anthracycline chemotherapy. PHARMACOLOGICAL & MECHANISM OF ACTION:- Arsenic has been a traditional poison for ages. Ehrlich produced oraganic arsenicals for cure of syphilis,and some organic arsenicals were used in amoebiasis till 1960s. Recently, therapeutic value of small doses of arsenic trioxide in APL has been recognized . It probably acts by enhancing reactive oxygen free radical generation in APL cells . It is primarily used in resistant/ relapsed cases of APL after tretinoin treatment. Lately ,arsenic trioxide is also being included in the 1st line therapy of APL along with tretinoin+ an anthracycline, particularly in high risk cases and in those who have initial WBC count of > 10,000/uL. With such triple therapy ...

ARMODAFINIL

 ARMODAFINIL BRAND NAME:- Armod,waklert or many brands available in India. ARMODAFINIL is a congener of modafinil which has been recently approved for improving wakefulness in patients with obstructive sleep apnoea (OSA) ,SWD and narcolepsy. PHARMACODYNAMIC:- Armodafinil (R-(−)-modafinil) has pharmacological properties almost identical to those of modafinil (a mixture of R-(−)- and (S)-(+)-modafinil). The (R)- and (S)-enantiomers have similar pharmacological action in animals. Armodafinil has wake-promoting actions similar to sympathomimetic agents including amphetamine and methylphenidate, although its pharmacologic profile is not identical to that of the sympathomimetic amines. Armodafinil is an indirect dopamine receptor agonist; it binds in vitro to the dopamine transporter (DAT) and inhibits dopamine reuptake. For modafinil, this activity has been associated in vivo with increased extracellular dopamine levels. In genetically engineered mice lacking the dopamine transporter, m...

ARIPIPRAZOLE

 ARIPIPRAZOLE BRAND NAME:- ABILIFY ,ARIPRA,ARILAN,BILIEF 10,15mg tabs, ARIVE 10,15,20,30mg tabs. ARIPIPRAZOLE is an antipsychotics is unique in being a partial agonist at D2 and 5-HT 1À receptor, but antagonist at 5- HT2 receptor. The high affinity but low intrinsic activity of aripiprazole for D2 receptors impedes dopaminergic transmission by occupying a large fraction of D2 receptors but activating them minimally . It is not sedation,may even cause insomnia. PHARMACODYNAMIC:- Aripiprazole has high affinity for serotonin type 2 (5HT2), dopamine type 2 (D2), alpha1 and 2 adrenergic, and H1 histaminergic receptors. It also acts on a number of other receptors with lower affinity. The exact method by which aripiprazole's action on these receptors translates to a clinically relevant effect is not yet known. MECHANISM OF ACTION:- The antipsychotic action of aripipra byzole is likely due to the agonism of D2 and 5-HT1A receptors though the exact mechanism has not been defined. Some adver...

ARGATROBAN

 ARGATROBAN BRAND NAME:- no specific brand available. ARGATROBAN is a synthetic direct thrombin inhibitor used for the prevention and treatment of thrombosis related to heparin use. PHARMACOLOGICAL ACTION:- Argatroban is a synthetic nonpeptide compound which binds reversibly to the catalytic site of thrombin,but not to the substrate recognition site. As such ,it produces a rapid and short lasting antithrombin action .That is approved in the USA, the EU and Japan for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT), and for anticoagulation of HIT patients undergoing PCI.  MECHANISM OF ACTION:- Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation. Administered by i.v . Infusion,it can be used in place of lepirudin for short - term indication in patients with heparin-induce...

ARECOLINE

 ARECOLINE BRAND NAME:-  no specific brand available  ARECOLINE is an alkaloid obtained from betel nut areca catechu and has muscarinic as well as nicotinic actions, including those on skeletal muscle endplate. It also has prominent CNS effect: has been tried in dementia as an enhancer of cognitive function, but not found useful — has no therapeutic use. PHARMACOLOGICALLY:- Arecoline is the primary active ingredient responsible for the central nervous system effects of the areca nut. Arecoline has been compared to nicotine; however, nicotine agonizes nicotinic acetylcholine receptors, whereas arecoline is primarily a partial agonist of muscarinic acetylcholine receptors,leading to its parasympathetic effects. In frogs, arecoline also acts as an antagonist (or very weak partial agonist) at α4 and α6-containing nicotinic acetylcholine receptors and as a silent antagonist at α7 nicotinic receptors, which may account for its anti-inflammatory activity.Arecoline also inhibits ...

ARDEPARIN

 ARDEPARIN BRAND NAME:- INDEPARIN 2500 IU ,5000 IU Prefilled syringes . ARDEPARIN is a low molecular weight (LMW) anticoagulant used for the prevention of postoperative venous thrombosis.Ardeparin is derived via peroxide degradation of heparin extracted from porcine intestinal mucosa. Its molecular weight ranges from 2000 to 15,000 with an average molecular weight of 5500 to 6500. PHARMACODYNAMIC:-  Ardeparin, an anticoagulant, is a fractionated heparin. It acts at multiple sites in the normal coagulation system to inhibit reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo.  MECHANISM OF ACTION:- Ardeparin has been fractionated into LMW forms (MW 3000-7000) by different anticoagulants profile; i.e. selectively inhibits factor Xa with little effect on IIa. Ardeparin binds to antithrombin III, accelerating its activity in inactivating factor Xa and thrombin, thereby inhibiting thrombosis. Ardeparin also binds to heparin ...

APREPITANT

 APREPITANT BRAND NAME:- APRECAP, APRESET ,APRELIFE ,EMPOV 125mg (one cap) + 80mg (2caps) kit. APREPITANT is a medication used to manage and treat chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV). It is in the neurokinin-1 antagonist class of medications.  PHARMACOLOGY & MECHANISM OF ACTION:-  It is a recently introduced selective , high affinity NK1 receptors antagonist that blocks the emetic action of substance P, with little effect on 5 HT3 and D2 or other receptors. Gastrointestinal motility is not affected. Oral aprepitant (125 mg + 80 mg + 80 mg over 3 days) combined with standard i.v. ondansetron+ dexamethasone regimen significantly enhanced the antiemetic efficacy against high emetogenic cisplatin based chemotherapy. Greater additional protection was afforded against delayed vomiting than against Acute vomiting. It was particularly useful in patients undergoing multiple cycles of chemotherapy. Adjuvant benefits of ap...

APRACLONIDINE

 APRACLONIDINE BRAND NAME:- ALFADROPS DS 1% eyedrops  APRACLONIDINE  also known as iopidine ,   It is an alpha2-adrenergic agonist. An alpha adrenergic agonist used to treat raised intraocular pressure.  PHARMACODYNAMIC:- Apraclonidine is a sympathomimetic. It works by decreasing the production of aqueous humour (fluid in the eye), thereby lowering the increased eye pressure.  Apraclonidine significantly lowers intraocular pressure with minimal effects on cardiovascular and pulmonary parameters. It lowers intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow. MECHANISM OF ACTION:- It is a polar clonidine congener which does not cross blood - brain barrier,but applied topically (0.5-1%) it lowers i.o.t. by - 25% . It decreases aqueous production by primary alpha2 and subsidiary alpha1 action in the ciliary body. Apraclonidine is a relatively selective alpha2 adrenergic receptor agonist that stimulates alpha1 receptors t...

APOMORPHINE

 APOMORPHINE BRAND NAME:-Zyprima 2-3mg ,SL tablet etc. APOMORPHINE is a semisynthetic derivative of morphine; acts as a dopaminergic agonist on the CTZ . Used to treat hypomobile "off" episodes of advanced Parkinson's disease.  PHARMACODYNAMIC:-  It is a semisynthetic derivative of morphine; acts as a dopaminergic agonist on the CTZ. Injection i.m./s.c in a dose of 6 mg ,it promptly (within 5 min) induced vomiting. It should not be used if resipration is depressant actions. Oral use of APOMORPHINE is not recommended because the emetic dose is larger ,slow to act and rather inconsistent in action. Apomorphine has a therapeutic effects in Parkinosonism,but is not used to side effects. MECHANISM of ACTION:- Apomorphine is a non-ergoline dopamine agonist with high binding affinity to dopamine D2, D3, and D5 receptors. Stimulation of D2 receptors in the caudate-putamen, a region of the brain responsible for locomotor control, may be responsible for apomorphine's action. Ho...

ANTI - HELICOBACTER PYLORI DRUGS

 ANTI - HELICOBACTER PYLORI DRUG  BRAND COMBINATION AVAILABLE:-  HP- KIT, HELIBACT ,OMXITIN :-omeprazole 20mg 2 cap + Amoxicillin 750mg 2 tab + tinidazole 500mg 2 tab. PYLOMOX : Lansoprazole 15mg 2 cap + Amoxicillin 750mg 2tab + Tinidazole 500mg 2 tab . LANSI KIT :- Lansoprazole 30mg 1 cap+ Amoxicillin 750mg 1 tab + Tinidazole 500mg 1 tab ( one kit twice a day) PYLOKIT, HELIGO : Lansoprazole 30mg 2cap + Clarithromycin 250mg 2 cap + Tinidazole 500mg 2 tab. LANPRO AC:- Lansoprazole 30mg 2 cap + Clarithromycin 250mg 2 tab + Amoxicillin 750mg 2 tab . It is an antimicrobial (triple, quadruple drugs) drug . Antimicrobial that are used clinically against H.pylori are:- Amoxicillin, Clarithromycin, tetracycline and metronidazole/ Tinidazole. Any single antibiotic is ineffective. H.pylori is agents used in treatment of Helicobacter Pylori are medicines used for stomach acid inhibition, combined with antibacterial agents. Treatment is for one week with a proton pump inhibitor or an...

ANTHRAQUINONES

 ANTHRAQUINONES BRAND NAME:- GLAXENNA 11.5 mg tab; PURSENNID 18mg tab; SOFSENA 12mg tab. ANTHRAQUINONES (also known as anthraquinonoids) are a class of naturally occurring phenolic compounds based on the 9,10-anthraquinone skeleton, are the plant products Used in household/ traditional medicine for centuries. PHARMACODYNAMIC & FUNCTION:- senna is obtained from leaves and pods of certain cassia sp., While Cascara sagrada is the powdered bark of the buck - thorn tree. These and a number of other plant purgatives contain ANTHRAQUINONES glycosides, also called emodins. Senna is most popularly used. The glycosides are not active as such . Unabsorbed in the small intestine,they passed to the colon where bacteria liberate the active anthrol from ,which either acts locally or is absorbed into circulation excerted in bile to act on small intestine. Thus they take 6-8 hours produce action . Taken by lactating mothers,the amount secreted in milk is sufficient to cause purgation in the suc...

Know details about ANIDULAFUNGIN drug ?

 ANIDULAFUNGIN  BRAND NAME:- ECALTA 50mg/vial, 100mg/vial etc many other brands available in India. ANIDULAFUNGIN is an anti-fungal drug & are the other echinocandins with similar properties. It was previously known as LY303366.  PHARMACODYNAMIC:- Anidulafungin is a semi-synthetic lipopeptide synthesized from a fermentation product of Aspergillus nidulans. Anidulafungin is an echinocandin, a class of antifungal drugs that inhibits the synthesis of 1,3-β-D-glucan, an essential component of fungal cell walls. Anidulafungin is active in vitro against many Candida, as well as some Aspergillus. Like other echinocandins, anidulafungin is not active against Cryptococcus neoformans, Trichosporon, Fusarium, or zygomycetes.  MECHANISM OF ACTION:- Anidulafungin is a semi-synthetic echinocandin with antifungal activity. Anidulafungin inhibits glucan synthase, an enzyme present in fungal, but not mammalian cells. This results in inhibition of the formation of 1,3-β-D-glucan, ...

Know details about ANDROSTERONE drug ?

 ANDROSTERONE BRAND:- ANDROSTERONE tablet,no specific brand available. ANDROSTERONE is a type of chemical known as an anabolic steroid. It is converted in the body to testosterone and other sex hormones. Pharmacodynamic:-  🚫 Not available. Mechanism of action:-  Androsterone, a neurosteroid, acts as a positive allosteric modulator of GABA(A) receptors, that can cross into the brain and could have effects on brain function. It was discovered, that the association of beta subunits with alpha subunits GABA(A) receptor affects the sensitivity of glycine receptors to androsterone. In spite of that, androsteron is considered as an inactive metabolite of testosterone. In addition, was studied that androsterone possessed anticonvulsant properties. Although of low potency, the androsterone was present in high abundance and was able to represent endogenous modulator of seizure susceptibility.  USED:- Androsterone is used for weight loss, to improve athletic performance, to re...

ANASTROZOLE

To ANASTROZOLE BRAND NAME:- ALTRAZ,ARMOTRAZ ,ANABREZ 1mg tab. ANASTROZOLE   another nonsteroidal and reversible (type 2) aromatase inhibitors (AI) , more potent than letrozole and suitable from single daily dosing.  ACTION:- Anastrozole is an aromatase inhibitor. It works by lowering the amount of estrogen (natural female hormone) produced in the body. This can lower or stop the growth of some breast cancer cells that need estrogen to grow. It accumulates in the body to produce peak effects after 7-10 days . Anastrozole is useful as adjuvant therapy in early ER+ I've breast cancer as well as for palliation of advanced cases in postmenopausal women. In early cases, tumor recurrence time was found to be longer than with tamoxifen. Risk of new tumor appearing in the contralateral breast was also lower with anastrozole. A longer time to disease progression compared to tamoxifen has been obtained in advanced ER + ve breast cancer. Many tamoxifen resistance cases responded with...

ANANDAMIDE (ANA)

 ANANDAMIDE(ANA) BRAND NAME:-  ANANDAMIDE also known as N- arachidonoylethanolamine 20:4 (AEA) is a fatty acid neurotransmitter. Resulting from the formal condensation of carboxy group of arachidonic acid with the amino group of ethanolamine. It has a role as a neurotransmitter, a vasodilator agent and a human blood serum metabolite. It is an endocannabinoid and a N-acylethanolamine 20:4. It is functionally related to an arachidonic acid.    FUNCTION:-  Anandamide is a lipid mediator that acts as an endogenous ligand of CB1 receptors. These receptors are also the primary molecular target responsible for the pharmacological effects of Δ 9-tetrahydrocannabinol, the psychoactive ingredient in Cannabis sativa.  Anandamide was the first endocannabinoid to be discovered: it participates in the body's endocannabinoid system by binding to cannabinoid receptors, the same receptors that the psychoactive compound THC in cannabis acts on. Anandamide is found in nearly ...

ANAKINRA

 ANAKINRA BRAND NAME:- kineret & others brand available in India. ANAKINRA is a recombinant human IL -1 receptors antagonist. Though clinically less effective than TNF inhibitors,it has been used in cases who have failed on one or more DMARDs.  PHARMACODYNAMIC:- stimulated macrophages and other mononuclear cells elaborate IL-1 which activated helper T-cells and induces production of other ILs, metalloproteinases ,etc. An endogenous IL-1 receptor antagonist has been isolated and several of its recombinant variants have been produced for clinical use. MECHANISM OF ACTION:- This recombinant human IL -1 receptors antagonist prevents IL-1 binding to its receptors and has been approved for use in refractory rheumatoid artritis not controlled MTx has been used alone as well as added to TNFalpha antagonist, because it's clinical efficacy as monotherapy appears to be lower. USE:- treatment of rheumatoid arthritis, cryopyrin-associated periodic syndromes, familial Mediterranean feve...

AMRINONE (INAMRINONE) ; used, Side effects, dose, pharmacodynamic & Mechanism of action.....

 AMRINONE (INAMRINONE) 

AMPHETAMINES

 AMPHETAMINES BRAND NAME:- ADDERALL,ADZEnys etc.. many brands available in India. Amphetamine is a powerful stimulator of the central nervous system . The central actions of amphetamines are largely medicated by release of NA from adrenergic neurones in the brain. Indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD). PHARMACODYNAMIC ACTION:-  These are synthesis compounds having a Pharmacological profile similar to ephedrine; it has been demonstrated that amphetamine augments the concentration of noradrenaline in the prefrontal cortex and dopamine in the striatum on a dose and time-dependent manner. The indistinct release of neurotransmitters which include adrenaline is known to produce cardiovascular side effects. There are old reports of a cognitive enhancement related to the administration of amphetamine in which improvements in intelligence test scores were reported. In ADHD, amphetamine has been largely showed to produce remarkable improvements i...

AMOXAPINE

 AMOXAPINE BRAND NAME:- Amoxipaine tab,DEMOLOX 50,100mg tab. etc many brands available in India. Amoxapine is in a class of medications called tricyclic antidepressants (TCAs). It works by increasing the amounts of certain natural substances in the brain that are needed to maintain mental balance.  ACTION:- This tetracycline compound is unusual in that it blocks  dopamine D2 receptors in addition to inhibiting NA reuptake . It is chemically related to the antipsychotics drug loxapine and has mixed antidepressant+ neuroleptics properties — offers advantage for patients with psychotic depression.  USED:- in symptoms of depression. SIDE EFFECTS:- risk of extrapyramidal is also there. Seizures ( including status epilepticus ) occur in its overdose.  DOSE:- 100-300mg daily.

AMMONIUM CHLORIDE

 AMMONIUM CHLORIDE BRAND NAME:- Damylin with codeine ,Acidex many brands available in India. Ammonium chloride is an inorganic compound with the formula NH4Cl. It is highly soluble in water producing mildly acidic solutions.  PHARMACOLOGICAL ACTION:- Systemic acidifier. In liver ammonium chloride is converted into urea with the liberation of hydrogen ions ( which lowers the pH) and chloride. Ammonium Chloride works by decreasing the stickiness of mucus (phlegm) and helps in its removal from the airways.  MECHANISM OF ACTION:- Ammonium chloride increases acidity by increasing the amount of hydrogen ion concentrations.Ammonium chloride can be used as an expectorant due to its irritative action on the bronchial mucosa. This effect causes the production of respiratory tract fluid which in order facilitates the effective cough. USE:-  as a expectorant, treatment of cough and mucus. SIDE EFFECTS:- Facial swelling, Allergic reaction, Difficulty in swallowing, Feeling sick, ...

AMISULPIRIDE

 AMISULPIRIDE BRAND NAME:- SULPITAC ,AMIPRIDE,ZONAPRIDE 50,100,200mg tabs. AMISULPIRIDE is an antiemetic and typical antipsychotic , m edication used at lower doses intravenously to prevent and treat postoperative nausea and vomiting. ACTION:- Amisulpiride  is a congener of sulpiride is categorized with the atypical antipsychotics because it produces few extra pyramidal side effects and improves many negative symptoms of schizophrenia as well. However,it retains high affinity for D2 and D3 receptors and has low-affinity for 5- HT 2 receptors. Hyperpolactinemia occurs similar to typical neuroleptics. Antidepressant property has been noted. Amisulpiride is not a sedative . USE:- Treatment of Acute and chronic schizophrenic disorders. Treatment of  postoperative nausea and vomiting. SIDE EFFECTS:- Rather, insomnia, anxiety and agitation. Risk of weight gain and metabolic complication is lower . DOSE:- 50-300mg/day in 2 doses for schizophrenia with predominant negative sympto...

AMINOPHYLLINE

 AMINOPHYLLINE BRAND NAME:-AMINOPHYLLINE 100mg tab ,250mg /10ml inj . AMINOPHYLLINE is water soluble & is a  bronchodilator consisting of theophylline that is used for the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis. PHARMACOLOGICAL ACTION:- Aminophylline is the ethylenediamine salt of theophylline. Theophylline stimulates the CNS, skeletal muscles, and cardiac muscle. It relaxes certain smooth muscles in the bronchi, produces diuresis, and causes an increase in gastric secretion.  MECHANISM OF ACTION:- Aminophylline is the ethylenediamine salt of theophylline. After ingestion, theophylline is released from aminophylline, and theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in sm...

AMINEPTINE

 AMINEPTINE BRAND NAME:-SURVECTOR  100mg tab. AMINEPTINE like tianeptine it enhances 5-HT uptake,and has antidepressant property. MECHANISM OF ACTION:-  Amineptine is an atypical tricyclic antidepressant.Amineptine selectively inhibits the reuptake of dopamine and to a lesser extent norepinephrine, thus exerting a powerful and fast-acting antidepressant effect. USED:- Treatment of depression. SIDE EFFECTS:- It produced anticholinergic side effects including tachycardia, confusion and delirium. Postural hypotension, conduction distrubance and arrhythmias can occur, especially in patients with heart disease. DOSE:- 100mg BD at breakfast and lunch.