Sunday 5 April 2015

Proteasomes



Proteasomes are protein complexes inside all eukaryotes and archaea, and in some bacteria. In eukaryotes, they are located in the nucleus and the cytoplasm. The main function of the proteasome is to degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Enzymes that carry out such reactions are called proteases. Proteasomes are part of a major mechanism by which cells regulate the concentration of particular proteins and degrade misfolded proteins.

Proprietary name ,Non-proprietary names and IUPAC names



Trade name,brand name , proprietary name are synonyms. .

Non-proprietary names are short names given to chemical or drug substances and are recognized by government agencies and other organizations.

Paracetamol and acetaminophen are non-proprietary names.

An International Nonproprietary Name (INN) ia an official non proprietary or generic name given to pharmaceutical drug ,as designated by the World Health Organization(WHO).

Acetaminophen is the name adopted in the U.S(USAN-U.S approved names) and Japan whereas,paracetamol is approved in a variety of international venues (INN,AAN,BAN etc)

The IUPAC nomenclature of organic chemistry is a systemic method of naming organic chemical compounds as recommended by the International Union of Pure and Applied chemistry.


The IUPAC books are the complete list of definitions maintained by the International Union of Pure and Applied Chemistry.
Nomenclature of Organic Chemistry commonly referred to by chemists as the Blue Book, is a collection of recommendations on organic chemical nomenclature published at irregular intervals by the International Union of Pure and Applied Chemistry (IUPAC).




Dosage form and Formulation


Tablet,capsules,injection are different dosage forms.Depending upon the stability of the drug ,its absorption in the body etc.drug is formulated in one of these forms.

Dosage forms contain 2 components 
1.Drug
2.Excipients

Example: 
Crocin(500mg) Tablet contains 500mg(strenght) of drug ie Paracetamol/acetaminophen ,but when you weight the tablet its weight will be  500-600mg,this extra 100mg is because of excipients .

 Formulation is not always disclosed by the company.
If you check on Benadryl cough syrup bottle you will find 
EACH 5 ml contains
Diphenhydramine HCl    14.08mg
Ammonium chloride      138mg
Sodium citrate                 57.03mg
Ethanol                            .2625ml
colours: carmoisine,sunset yellow ,FCF,Erythrosine,Caramel I.P

This can give you a rough idea about formulation .
In case of Benadryl ,Diphenhydramine HCl is the Drug and all the other substances are excipients.The quantity of excipients can be more than that of drug .

Crocin(Glaxo Smithkline) and Benadryl (Johnson & Johnson) are proprietary names(trade names) under which a manufacturer  markets its product.The drug in crocin is Paracetamol/amphetamine and in Benadryl is Diphenhydramine HCl.

Tylenol also contains 500mg paracetamol .The brand name "Tylenol" is owned by McNeil Consumer Healthcare, a subsidiary of Johnson & Johnson.

Saturday 3 January 2015

Drug and Excipient

Drug and Excipient

Drug is the active ingredient and excipients are inactive ingredients of a formulation.

Excipients could be binders,lubricants,coating,preservatives,sweeteners etc..depending on the nature of drug.
The excipients should not react with the drug ,interaction between drug and excipients might cause loss of drug activity or other unfavorable reactions.
Behind a tablet or capsule strip or on the bottle of a syrup the drug name and its quantity is printed .








Tuesday 23 December 2014

In-vivo preclinical test for antiepileptic drugs



Maximal electroshock seizure (MES)
In the MES test, mice or rats receive an electrical stimulus of sufficient intensity to induce maximal seizures of their hind limbs, with tonic extension as the endpoint of the test
In the MES test,60Hz alternating current is delivered for 0.2 second through corneal electrodes.
The test is easily conducted, requires a minimal investment in equipment and technical expertise, and is well standardized. Additionally,the epileptic activity is no longer contaminated by the epileptogenic agent since it occurs only during application of the current.
Unfortunately, the animals can be used only once.

 6-Hz Seizure Test
Compounds are also screened for their ability to block psychomotor seizures induced by a low-frequency (6 Hz), long-duration (3 sec) stimulus delivered through corneal electrodes
6 Hz test demonstrates partial, to complete resistance to the Na+ channel blockers, thus making the 6 Hz test useful as an early identification and differentiation screen.
Compounds found to be effective in this low-frequency (6 Hz), long-duration assay may therefore be effective in the treatment of therapy-resistant partial seizures. 

Subcutaneous Metrazol (sc Met)
Subcutaneous injection of the convulsant Metrazol produces clonic seizures in laboratory animals.
The scMET test detects the ability of a test compound to raise the seizure threshold of an animal and thus protect it from exhibiting a clonic seizure in response to a normally convulsant dose of Metrazol.
Animals are pretreated with various doses of the test compound given by i.p. injection or through oral dosing. At various times after dosing with the test compound, the dose of Metrazol which will induce convulsions in 97% of animals is injected into a loose fold of skin in the midline of the neck.
The animals are placed in isolation cages to minimize stress and observed for the next 30 minutes for the presence or absence of a seizure.
 An episode of clonic spasms, approximately 3-5 seconds, of the fore and/or hindlimbs, jaws, or vibrissae is taken as the endpoint.
 Animals which do not meet this criterion are considered protected