Intro To Basic Conceptd And Definition In Pharmacokinetics Flashcards
Drug metabolism takes place in ***
Gi tract
Skin
Lungs
Kidney
Liver
Cytochrome p450 accounts for …….. % of phase 1 metabolism of drug
95%
90% of cyp450 metabolism of drug is carried out majorly by the following enzymes
Cyp1A2
Cyp2C9
Cyp2C19
2D6
3A4
List other enzymes involved in phase 1 of drug metabolism
Monoamine oxidises which metabolises catecholamines
Alcohol dehydrogenase which metabolises alcohol including methanol
Metabolism of of alcohol produces toxic substances such as
Formaldehyde
The primary method of Microsoft enzyme induction is…………
Transcription
Carbamezapine is a substrate and inducer of ………..
CYP 3A4
Carbamezapine induces and out 50 %of drugs if coadministered with it like …………..
Rifampicin and saquinavir
What are orphan receptors
They are receptors whose ligand is currently unknown
List the classes of receptor protein
Regulatory protein( most characterized)
Enzyme( mostly inhibited and less commonly activated)
Transport protein
Structural protein e.g tubulin
The transduction process that links drugs occupancy of receptors and pharmalogical response is called
COUPLING
The efficiency of occupancy-response
Couplig is determination by
The initial conformational change
The degree of spareness of a receptor is…….
The total number of receptors present compared with the number of receptors required to elicit a maximal biological response
Transmembrane receptors intracellular domain can be:
Tyrosine kinase
Serine kinase
Guanylyl kinase
Transmembrane receptors intracellular domain can be:
Tyrosine kinase
Serine kinase
Guanylyl kinase
When clearance is first order it can be calculate by
Calculating area under the curve(AUC)
What I’d the half life of a drug
It is time taken to reach 50% of steady-state or decay 50% from steady steady after a change in drug admission
Acid drugs and basic drugs are bound to which Plasma protein respectively
Albumin
Alpa 1 acid glycoprotein or lipoprotein
Most drugs are between ………. size to…….
250 to 450 Da MW
What is pharmacology?
This is the study of substances that react chemically with the body, by binding with a regulatory molecule and brings about a response by activating or inhibiting body response
List and explain two drugs that binding through covalent bond
Aspirin
Alkylating agent
Describe the the three modes in which a drug receptor bond brings about an effect
D+R stuff
What is the constitutive activity of receptors
This the a state in which some receptors remain in the Ra active state and induce physiological response even in the absence of agonist
What is intrinsic efficacy?