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Showing posts with the label Pharmacology

Vasomotor reversal of dale

A very simple explanation for vasomotor reversal of Dale Adrenaline/Epinephrine: Blood pressure changes has biphasic response  Initially adrenaline concentration is high: acts on both alpha and beta receptors  Alpha action predominates resulting in vasoconstriction and increase in BP  Adrenaline action is rapidly reduced due to uptake and metabolism  At lower concentrations: beta action predominates  Resulting in vasodilation and reduction in BP  Vasomotor reversal of Dale  Phenoxybenzamine abolishes biphasic response  As alpha receptors are blocked; blood pressure only falls (beta receptors)

Pharmacokinetics of Chloroquine

Rapidly and completely absorbed by oral route Very large volume of distribution: loading dose is necessary Concentrated in erythrocytes, liver, spleen, kidney, lung, melanin-containing tissues Retina accumulation: ocular toxicity on long term use Partly metabolised by hepatic mixed function oxidase system Metabolites and parent drug excreted in urine

Difference between bioequivalence and therapeutic equivalence

Bio equivalence Different pharmaceutical companies in the world can prepare same compounds with same dosage forms If two or more similar dosage forms of same drugs reach the blood circulation at same rate then those preparations are called bioequivalent products If the difference in bioavailability of the preparation is less than 20% these are known to be bioequivalent The drug regulatory authorities asks for bioequivalent study report when a pharmaceutical company applies for ANDA filing   Therapeutic equivalence Structurally different drug can provide the same clinical response as another drug then it is called as therapeutically equivalen ce All bioquivalent drugs are therapeutic equivalent but the converse is not true.  

BIOEQUIVALENCE

Different pharmaceutical companies in the world can prepare same compounds with same dosage forms If two or more similar dosage forms of same drugs reach the blood circulation at same rate then those preparations are called bioequivalent products If the difference in bioavailability of the preparation is less than 20% these are known to be bioequivalent The drug regulatory authorities asks for bioequivalent study report when a pharmaceutical company applies for ANDA filing  

Bleeding associated with cephalosporins is because of the side chains interfering with prothrombin synthesis

Some cephalosporins have been associated with bleeding complications. It may be due to hypoprothrombinaemia and/or platelet dysfunction occurring with cephalosporins and cephamycins having an N-methylthiotetrazole side-chain, including • cefamandole • cefbuperazone • cefmenoxime • cefmetazole • cefonicid • cefoperazone • ceforanide • cefotetan • cefpiramide • latamoxef. The presence of a methylthiadiazolethiol side-chain in cefazolin, or an N-methylthiotriazine ring in ceftriaxone, might also be associated with such bleeding disorders. Hypoprothrombinaemia is usually reversible with vitamin K. It was previously thought to be due to an alteration in intestinal flora but interference with prothrombin synthesis now seems more likely.

Monocloncal antibody approved for hypercholesterolemia. Is it the next big thing after stains?

The U.S. Food and Drug Administration on Friday approved alirocumab, the first of a new class of injected, cholesterol-lowering drugs. Alirocumab cuts levels of LDL cholesterol, and is one of a group of newly developed drugs called PCSK9 inhibitors. The molecule happens to be a monoclonal antibody. Approved indications  The drug is only approved for patients with heart disease and a history of heart attack or stroke "who require additional lowering of LDL cholesterol" in addition to taking a statin drug and adopting a healthy diet.  Heterozygous familial hypercholesterolemia (HeFH), an inherited illness that causes people to have high levels of LDL in the blood.  The video shows how this new class of drugs reduces LDL levels in blood.  >

Modern medicine : misconceptions in terminology of allopathy and drugs

Allopathy The modern medicine is wrongly termed as Allopathy by many. The term Allopathy stands for "the other suffering". The term was coined when the likes of James Gregory were doing irrational treatment which consisted of using high doses which created a new suffering which was far worse than the initial suffering. Modern medicine is thoroughly rational and aims at reducing the initial suffering without causing additional suffering. Drug The word "Drug" has its origin from French; drug = drogue; a dry herb. Many of us have a misconception that drugs prescribed are usually synthetic and are non natural products. Many of the drugs and the word drug itself has it's origin in herbs. The difference now is we know the exact active ingredient and it's action. Drugs are now highly specific in action and are introduced based on valid experimentation.

Salvarsan : the beginning of the chemotherapy

Paul Ehrlich's obsession about using dyes for treating diseases culminated into the creation of product called arsphenamine. Arsphenamine, though too toxic was used to treat Syphilis as no other drug existed then. The product was patented as Salvarsan - touted to be a salvation for all human sufferings. The Salvarsan points at the era of beginning of systematic approach at discovering drugs. Next came an another dye, prontosil, by Gerhard Domagk which essentially began the era of chemotherapy.

Heparin Mechanism of Action

India bans pioglitazone : The impact

Widely prescribed anti-diabetes drug pioglitazone and its combinations were banned on June 26 by Governemnt of India. Along with this, painkiller analgin and anti-depressant deanxit(Flupenthixol+ Melitracen) were also banned under Section 26A of the Drugs and Cosmetics Act(1940) by ministry of health and family welfare, India. Pioglitazone's safety : Always a concern   Pioglitazone is an anti-diabetic drug, which has unique action on improving insulin resistance by acting on PPAR receptors. Studies have reported pioglitazone causes congestive heart failure due to fluid retention and also bladder cancer. It also causes   muscle aches, headache, nausea, vomiting, loss of appetite, pain in the abdomen etc. Three years ago another drug from this family, rosiglitazone was banned in India following a decision taken in European Union.   Following the reports of adverse effects, France has discontinued Pioglitazone, but USA and UK allowed restricted use of Pioglitaz...

Cytochrome enzymes nomenclature

Cytochrome : CYP Followed by family in numbers like 3 Subfamily indicated by capital letters like A Isoenzymes again by numbers like 4

Nice story to remember about antimalarial drugs...

The anti malarial drugs is one such thing where recalling the names itself is like repeating a tongue twister. But here is a story which helps to retain the important points about the mechanism, adverse effects, uses of these drugs. Antimalarials: The Harem Once upon a time in a parallel Universe, there was a swampy kingdom ruled by King Medico. So, the story goes that once the kingdom was attacked by an epidemic of Malaria (Attack of the Plasmodia). The King (who is you in this story) decided to send his Queens out to destroy Malaria (much like in Chess: the Queen goes out to destroy, the King sits at home and watches ESPN!) He had 10 queens (including one eunuch), a mafia couple, a cyclist-warrior, a new warrior, and a CIA agent. Chloe-Queen (Chloroquine). Right, so…Chloe the Queen was a pretty effective warrior; she fought fast and long. The parasites had occupied the Temples of the Red Corpuscles and were trying to degrade the sacred substance Heme, but she complexed with Heme an...

Probenecid and penicillin combination explained in animation