Pharmacology-Ser Loisse Mortel.pdf

 

3

SLRM2014 (no affiliation with the STC)

ACTIONS OF RECEPTORS

It is in addition prudent to discuss where the genuine active sites are and what the receptors prepare to know which drugs in ~issimo can act on them. Again, receptors can be a)

 

Regulatory

 

 –

 have the direction of the functions of a body and either activates or inhibits such function b)

 

Enzymatic

 

 –

 speeds up a chemical reaction essential for the body c)

 

Structural

 

 –

 builds up a instance cell, tissue, or organ in the body d)

 

Transport

 

 –

 brings up a unquestionable essential element or compound through separate areas or parts of the body Active sites regulating drug action have power to fall under the following: a)

 

Intracellular

 

 –

 whither the drug acts inside the cell; oftentimes this involves transcription function, leave be slow to act

and moreover slow to lose effect (“move slowly times”)

 b)

 

Transcellular

 

 –

 to which place the active site as

embedded in a receptor’s simplest organism membrane;

i)

 

Ligand-gated

 

 –

 a single compound will open the receptor ii)

 

Voltage-gated

 

 –

 change in electrical potential around the receptor bequeath open it iii)

 

Secondary express-regulated

 – upon binding of a ligand, a G-protein resolution cause formation of molecules inside the solitary abode; squalid that perform the expected effect of physic; because these are created from another primary source, they are termed delegate messengers (ex. cAMP, cGMP, phosphoinositides IP3 and DAG) Original unsalable article function can be altered by the receptors (considered in the state of some form of adaptation) by regulating theirselves:

Downregulation

 

 –

 medicine-receptor complex with agonist exists in the way that often that receptors are tricked to function greater than normal, and they

vanquish

 in number – if the able to endure stops drug use then original entirely function is much lesser than first

Upregulation

 –

 drug-receptor web with antagonist exists so often that receptors are tricked to performance lesser than normal, and they

enlarge

in number – if the patient stops put ~s into use then original bodily function is abundant greater than original However, original put ~s into function may be altered by other ways: A)

Reduction of endogenous ligand

 –

 

suppose that a naturally occurring agonist is reduced in contain, antagonists will not give significant clinical furniture. B)

Reduction of drug in the stirring site

 –

 

can turn up due to increased metabolism of deaden with narcotics or reduction in absorbption by transporters that discharge the drug from the path towards the bloodstream C)

Biochemical changes

 –

 uniform if a constant amount of deaden with narcotics reaches the active site, binds constantly to a continuous number of receptors, the biochemical pathways and processes that the receptor controls may take defects in certain steps or enzymes.

CLINICAL PRACTICE Toxic prescribed portion

 

 –

 concentration at that 50% of subjects show signs of toxicity; signified being of the kind which TD

50

 

Lethal dose

 

 –

 for the most part same definition as toxic dose, this time killing a affix a ~ to of test subjects; LD

50

 

Therapeutic integral part

 

 –

 oftentimes LD

50

/ED

50

 (fowl of the air testing) or TD

50

/ED

50

 

(humans, since you’re not

supposed to carry off them lol) Drug interactions

 –

 any effect where one drug alters the purport of another a)

 

Additive

: 1 + 1 = 2 b)

 

Antagonism

 : 1 + 1 = 0 c)

 

Potentiation

: 1 + 0 = 2 d)

 

Synergism

: 1 + 1 = 3

Hyporreactive reponse

 

 –

 issue less than expected effect

Hyperreactive response

 

 –

 outcome greater than expected consequence

Tolerance

 

 –

 decreased answer to drug; can either be directly to downregulation or increased metabolism

Dependence

 

 –

 perpendicular body function is decreased because long-suffering needs drug for body to performance normally, oftentimes due to downregulation

Tachyphylaxis

 

 –

 actual quick tolerance

Cross-tolerance

 

 –

 deaden with narcotics that caused tolerance also gives long-suffering tolerance to other related or in like manner unrelated drugs

Withdrawal

 

 –

 oftentimes unwanted goods that come after one stops excitement a particular drug, especially if he is dependent on it.

Adverse drug event

 – anything that goes guilt when taking a drug at erect dosage or due to overdose.

Adverse mix with ~s reaction

 

 –

 a single one unintended, undesirable response to a put ~s into given at normal dosage during normal use. Types:

Augmented

 – related to remedy effects

Bizarre

 – unrelated to medicine effect

Chronic

 – due to prolonged employment of drug

Delayed

 – includes teratogenesis and carcinogenesis

End of manipulation

 – includes withdrawal effects

Failure of therapy

 – usually owed to ineffective prescription or ineffective unsalable article product

Hypersensitivity

 

 –

 inexpedient exaggerated reactions by the immune rule. It has four types:

I

 –

 Immediate/ IgE-mediated

 

Results from histamine, leukotriene, and prostaglandin absolution –

 

Urticaria, asthma, allergic rhinitis, anaphylaxis, angioedema

II

 –

 Cytotoxic/Antibody or fulness-dependent

 

Hemolytic anemia, thrombocytopenia, prejudicial anemia

III

 –

 Deposition of complexes in vessels or tissues

 

Systematic lupus erythematosus (SLE), rheumatoid arthritis, glomerulonephritis, serum complaint

IV

 –

 Cell-mediated/ Delayed hypersensitivity

 

Caused through sensitized T-lymphocytes –

 

Contact dermatitis, allograft declination, thyroiditis, Steven-Johnson syndrome, toxic epidermal necrolysis (TEN), tuberculin, erythema multiforme

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