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Showing posts with the label . Pharmacological

ATENOLOL / S(-) ATENOLOL

 ATENOLOL BRAND NAME:-BETACARD ,ATEN,TENORIM 25,50,100mg tab. Atenolol is a beta blocker having low lipid solubility.All beta blockers, irrespective of associated properties,exert similar antihypertensive effects.Drugs with intrinsic sympathomimetic activity (ISA) cause less/no reduction of HR and c.o. but lower vascular resistance by Beta2 agonism.   Medication primarily used to treat high blood pressure and heart-associated chest pain. Atenolol, however, does not seem to improve mortality in those with high blood pressure. Other uses include the prevention of migraines and treatment of certain irregular heart beats.   ATENOLOL is Cardioselectivity  drug , these are more potent in blocking cardiac Beta1 than bronchial Beta2 receptors.  CARDIOSELECTIVITY:- These drug are more potent in blocking cardiac Beta1 than bronchial Beta2 receptors. Selectivity is only relative and is lost at high doses.  Their features are:- 1. Lower propensity to cause br...

ATAZANAVIR (ATV)

 ATAZANAVIR(ATV) BRAND NAME:- ATAZOR 100,150,200,300mg caps. ATAZANAVIR is an antiviral and retroviral protease inhibitors (PIs) drug. An aspartic protease enzyme enclosed by HIV is involved in the production of structural proteins and enzymes of the virus from the large viral polyprotein synthesized in the infected cell. The polyprotein is broken into various functional components by the protease enzyme. It acts at a let step in HIV replication, i.e maturation of the new virus particles when the RNA genome acquires the core proteins and enzymes. PHARMACOLOGICAL & MECHANISM OF ACTION:- This PIs  is administered with light meal which improve absorption, while acid suppressant drugs decrease it's absorption. ATV is primarily metabolized by CYP3A4, which is also moderately inhibited by it. Bioavailability and efficacy of ATV is improved by combining with RTV . The t½ is 6-8 hours. Dyslipidaemia and other metabolic complicated are minimal with ATV , but jaundice occurs in some...

ARTESUNATE -PYRONARIDINE (1:3)

 ARTESUNATE -PYRONARIDINE(1:3) BRAND NAME:-   ZUNATE KIT OR etc. ARTESUNATE -PYRONARIDINE is an antimalarial and artemisinin Derivatives drug.  Pyronaridine is a water soluble naphthyridine Mannich base erythrocytic schizontocide with high efficacy and mechanism of action similar to CQ ,that has been used in China for -40 years. It is active against both CQ- sensitive and CQ- resistance P. falciparum and other malarial species. The onset of action is slower and duration long . It is concentration in RBCs and metabolized with a terminal t½ for 7days. Weak analgesic antipyretic action is produced at higher doses. Clinically efficacy of artesunate -PYRONARIDINE FDC (dose 1:3) has been tested in falciparum malaria in china, Thailand and Africa with > 95% success and no recrudescence in 28days. Multidrug resistant P.falciparam and P . Vivax also respond. Clinical trials have been completed in India 🇮🇳 with > 95% cure rates. Artesunate -PYRONARIDINE is well tolerat...

ANTI- TETANUS IMMUNOGLOBULIN (HUMAN) /TETANUS

 ANTI-TETANUS IMMUNOGLOBULIN (HUMAN) /TETANUS  BRAND NAME:- TETANUS ANTITOXIN 750IU,1500 IU,5000IU ,10,000 IU, 20000IU AND 50,000 IU in 1-10ml ampoules. TETANUS IMMUNE SERUM (enzyme refined, equine) 10,000 and 20,000 IU vials. TETANUS:- 1.TETANUS IMMUNO GLOBULIN (HUMAN) 2.TETANUS ANTITOXIN (ANTI-TETANUS SERUM,ATS) 1.TETANUS IMMUNO GLOBULIN (HUMAN) it is indicated for prophylaxis in non - immunized person receiving a contaminated wound who are at high risk of developing tetanus. The t½ of this ANTITOXIN is 4 weeks and significant blood levels are maintained for upto 14weeks . It is more efficacious and longer acting than the equine ANTITOXIN (ATS) . IF tetanus toxoid is given at the same time (but at a different site) , development of primary immune response to the toxoid is not interfered with. It has also been used for the treatment of clinical tetanus,but the efficacy is variable. Intrathecal administration has also been tried. DOSE:- Prophylactic 250-500IU , therapeutic 300...

ANTI- D IMMUNOGLOBULIN (HUMAN)

 ANTI - D IMMUNOGLOBULIN (HUMAN) BRAND NAME:-RHESUMAN ,RHOGAM, IMOGAM 300ug per vial / prefilled syringe. ANTI -D IMMUNE GLOBULIN is a human IgG having a high titer of antibiotics against Rh (D) antigen. It binds the Rho antigens and does not allow them to induce antibody formation in Rh negatives individuals.  It is miscellaneous immunosuppressant vaccine and SERA class drug. USED:- It is used for prevention of postpartum/post-abortion formation of antibodies in Rho-D negative, DU negative women who  have delivered or aborted an Rho- D positive,DU postive baby /foetus.  DOSE:- Administered with in 72 hours of delivery/absorption, such treatment prevents Rh haemolytic disease in future offspring. It has also been given at 28th week of pregnancy. 250- 350ug i.m. of freez dried preparation. Higher doses (1000-2000ug) are needed for Rh negatives recipients of inadvertently administered Rh positive blood.  NOTE:- IT SHOULD BE NEVER GIVEN TO THE INFANT OR TO Rho-D PO...

AMLODIPINE

 AMLODIPINE BRAND NAME:- AMLOPRES,AMCARD,AMLOPIN ,MYODURA 2.5,5,10mg tabs. AMLODIPINE is a class of calcium channel blocker , Dihydropyridined group drug. These Dihydropyridined (DHPs) are most potent Ca²+ channel blocker, and this subclass has proliferated exceptionally . The common property of CCBs is to inhibit Ca²+ mediated slow channel components of action potential (AP) in smooth) / cardiac muscle cells. The two most important action of CCBs are: 1. Smooth muscle (especially vascular) relaxation. 2. Negative chronotropic ,inotropic and dromotropic action of heart. Oral absorption is slow ,but complete; peak blood level occurs.after 6 to 9 hr -- the early vasodilator side effects (palpitation, flushing, headache, postural dizziness) are largely avoided. Because of less extensive and less variable first pass metabolism, its oral bioavailability is higher and more consistent. Volume of distribution and t½ are exceptionally long: diurnal fluctuation in blood level is small and ac...

ADENOSINE

 ADENOSINE BRAND NAME:- ADENOJECT, ADENOCOR 3mg adenosine (base) per ml in 2ml and 10ml amp. ADENOSINE administered by rapid i.v injection (over 1-3sec) either as the free base (6-12mg) or as ATP(Adenosine triphosphate) (10-20mg) , Adenosine terminates with in 30sec. More than90% episodes of PSVT involving the A-V node.it activated ACh sensitive K+ channels and causes membrane hyperpolarization through interaction with A1 type of Adenosine GPCRs on SA node (pacemaker depression ~bradycardia ), A-V node (prolongation of ERP--slowing of conduction ) and atrium (shortening of AP, reduced excita-bility). It indirectly reduces Ca2+ current in A-V node. Depression of the reentrant circuit through A-V node is responsible for termination of majority of PSVTs. Adrenergically  induced DADs(delayed after -depolarization) in ventricle are also suppressed. Coronary dilatation occurs transiently. ACTION:-adenosine has a very short T1/2 in blood (~10sec) due to uptake into RBCs and endotheli...

ACYCLOVIR used, dose, Side effects & more

 ACYCLOVIR BRAND NAME:- ZOVIRAX 200mg tab,250mg /vial for i.v inj ; CYCLOVIR 200mg tab , 5% skin cream; HEPREX 200mg tab, 3% eye oint, 5% skin cream; OCUVIR 200,400,800mg tab,3% eye oint,ACIVIR DT 200,400,800mg tab . ACIVIR EYE 3%oint. ACYCLOVIR the deoxiguanosine analogue antiviral drug requires a virus specific enzyme for conversion to the active metabolite that inhibits DNA synthesis and viral replication.  ACYCLOVIR is preferentially taken up the virus infected cells. Because of selective generation of the active inhibitors in the virus infected cells and it's greater inhibitory effects on viral DNA synthesis, ACYCLOVIR has low toxicity for host cells : a several hundred -fold chemotherapeutic index has been noted. ACYCLOVIR is active only against herpes group of viruses; HSV-1 is most sensitive followed by HSV-2 >VZV =EBV, while CMV is practically not affected. HSV and VZV have been found to develop resistance to acyclovir during therapy;the former primarily due to mut...

ACTIVATED CHARCOAL

 ACTIVATED CHARCOAL BRAND NAME:- Charcoal, Activated charcoal ACTIVATED CHARCOAL  has pores that can trap chemicals. It is typically  taken by mouth as a treatment for swallowed POISONs.  CHARCOAL are made from peat,coal,wood, coconut cell or petroleum . ACTIVATED CHARCOAL is made by heating charcoal in presence of a gas . This process cause the charcoal to develop lots of internal spaces or pores. These pore help ACTIVATED CHARCOAL to trap chemicals. USED:- Poison,it is also used for high cholesterol , hangover and upset stomach . BUT THERE IN NOT STRONG SCIENTIFIC EVIDENCE TO SUPPORT MOST OF THE USEs. WHEN APPLIED To the SKIN is LIKELY SAFE FOR MOST ADULT APPLIED TO WOUNDS. SIDE EFFECTS:-ACTIVATED CHARCOAL is  likely safe when used short term. Taking ACTIVATED CHARCOAL in long trem is possibly safe.  Common side effects including constipation and black stool. safe in PREGNANCY and BREAST FEEDING when used in short term. DOSES:- As medicine ACTIVATED CHARC...

Know details about ACETAZOLAMIDE drug ?

 ACETAZOLAMIDE BRAND NAME:-DAIMOX ,SYNOMAX 250mg tab,  IOPAR-SR 250mg SR cap.                         ACETAZOLAMIDE is a sulfonamide derivative which non -competitively but reversibly inhibits CAse (type II) in PT cells resulting in slowing of hydration of CO2 - decreased availability of H+ to exchange with luminal Na+ through the Na+-H+ antiporter. Inhibition of brush border CAse (type IV) retards dehydration of H2CO3 in the tubular fluid so that less CO2 diffuses back into cell. The net effect is inhibiton of HCÅŒ3 (and accompanying Na+) reabsorption in PT . However,the resulting alkaline diuresis is only mild (maximal fractional Na+ loss 5%), because part of the Na+ (but not HCÅŒ3) rejected in the PT is reabsorbed at the hight capacity AscLH.  Secretion of H+ in DT and CD is also interfered. Though H+ is  secreted at this site by a H+-ATPase , it is generated in the cell by CAse medicated reaction. As such,...