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General Pharmacology > Pharmaco-dynamics And Kinetics > Flashcards

Pharmaco-dynamics And Kinetics Flashcards

1
Q

Examples of weak acids

A 
Aspirin
Ibuprofen 
Acetazolamide 
Phenobarbital 
Methotrexate
Warfarin
APIM
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2
Q

Aspirin and ibuprofen are what type of drugs ?

A

NSAIDs and used as analgesics for musculoskeletal pain

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3
Q

What is phenobarbital used for?

A

Seizures and insomnia

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4
Q

What is acetazolamide used for?

A

Used for intraocular pressure and heart failure

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5
Q

What is TCA used for

A

They are used as antidepressants

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6
Q

What are weak basic drugs?

A
  • Codine
  • Atropine
  • cocaine
  • morphine
  • amphetamine
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7
Q

What are atropine used for?

A

They are used as cholinergic antagonists

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8
Q

What are codine and morphine used for?

A

They are used as analgesics for visceral pain

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9
Q

What substances can you use to acidify the urine to change urine ph?

A

NH4CL, Vitamin C, Cranberry juice

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10
Q

What substances can you use to alkalinize the urine to change urine ph?

A
  • NaHCO3 (sodium bicarbonate)
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11
Q

Acid drug + acidifying urine subs
Acid drug + alkalinizing urine subs (and vice versa)

Explain and give examples

A

Like and like- nonionised and absorbed

Opposites- ionized and eliminated

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12
Q

What oral drug has a 100% bioavailability’s

A

Isosorbide mono nitrate and it’s is used for heart-related chest pain, heart failure, and esophageal spasms.

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13
Q

Unbound drugs cross/does not cross bio-membranes

A

Unbound drugs cross bio-membranes. So the fraction of the drug in the plasma that is bound is inactive and generally unavailable for systemic distribution.

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14
Q

Acidic drugs to ——— in plasma while the basic drug binds to ———

A
  • plasma albumin
  • alpha 1 acidic glycoprotein

Other plasma binding proteins are: lipoprotein and cortisol binding globulin

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15
Q

What drugs are highly bound to plasma proteins?

A
  • OHA : Glipizide, Glimepride, Glyburide,
  • NSAIDs
  • sulfonamides s/e: recurrent diarrhea
  • cardiac glycosides: digoxin
  • Warfarin

CWONS

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16
Q

What are the formula for apparent volume of distribution

A

Total amount of drug in the body / plasma concentration of drug in the body

(Explain further)

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17
Q

Prodrugs and their examples

A

Drugs that become activated after bio-transformation

  • Monoxidil
  • Morphine
  • Dopamine
  • Prednisone
  • Epinephrine
  • Flurouracil
  • Sulfasalazine: 5aminosalylic acid
  • Zidovudine
  • Mecaptopurine
  • Cyclophosphaminde
  • methyl dopa
  • Clopidogrel
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18
Q

INH undergoes phase —— before phase —— during metabolism

A

Phase 2 before phase 1

It is first acetylated before hydrolyzed to isonicotinic acid

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19
Q

Alcohol could —— or —— cytochrome p450

A

Inhibit or induce

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20
Q

What are the substances or drugs that undergo non-microtonal reactions?

A
  • Amine Oxidation e.g cathecholamins or histamine
  • Alcohol dehydrogenation e.g ethanol oxidation
  • Esterases e.g pravastatin metabolisid in liver
  • hydrolysis e.g procaine
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21
Q

Explain the link between gray baby syndrome and chloramphenicol

A

Baby’s can’t produce enough glucoronic acid so less ionization and the accumulation of the drug.

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22
Q

What drugs undergo acetylation

A
  • statins: hyperlipidemia
  • Isoniazid: Tuberculosis
  • procainamide: arrhythmia
  • hydralazine: hypertension
  • monocycline: antibiotics

PHISM

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23
Q

Drugs that undergo sulfation

A

Steroids and minoxidil

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24
Q

What is the purpose of glutathione conjugation for acetaminophen

A

It helps to convert the toxic intermediate of acetaminophen (NAPBQI) to a non - toxic form (cysteine and mercapturic acid.

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25
Q

Where are the cyp450 isoenzymes located?

A

The SER of lungs liver GIT and kidney

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26
Q

What are the 3 isoenzymes of CYP 450?

A
  • CYP1A
  • CYP2D6
  • CYP3A4 ( common)
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27
Q

What is the substrate, inhibitors and inducers of CYP1A

A

Substrate: Theophylline
Inhibitors: Macrolides and fluoroquinolone
Inducers: aromatic hydrocarbons

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28
Q

What is the substrate, inducer and inhibitor of cyp2D6

A

Substrate: Codeine and metaprolol
Inhibitors: haloperidol and quinidine

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29
Q

What is the substrate, inducer and inhibitor of CYP3A4

A

Substrate: a wide range
Inducer: general cyp450 inducers
Inhibitor: Azoles, macrolides, acute alcohol intake, cimetidine

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30
Q

What are the general inducers of cyp450 enzyme?

A
  • phenobarbital
  • phenotoyin
  • chronic alcoholism
  • carbamazepine
  • rifampin
  • St. John wort

Sir Rifampin Can’t Come to our Private Property

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31
Q

What drug inhibits the cyp450 enzyme generally?

A
  • azoles
  • acute alcoholism
  • macrolides
  • cimetidine
  • cranberry juice
  • sodium valproate
  • omeprazole
  • ciprofloxacin
  • allopurinol
  • ritunavir
  • amiodarone
  • SSRI
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32
Q

——- is an autoinducer of CYP450 such that whatever it does affects itself.

A

Carbamazepine

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33
Q

Drugs that cause drug induced SLE

A
  • INH
  • Hydralazine
  • Statins
  • Procainamide
  • Phenytoin
  • Penicillamine
  • Quinidine

NHIS PQ

34
Q

What drugs increase the first pass effect?

A 
Lidocaine: anti arrhythmic 
Propanol: beta blocker 
Verapamil: Ca blocker
Aspirin: NSAIDS
Testosterone
Corticosteroids

(Very Poor Little CAT)

35
Q

What is the most common form of elimination?

A
  • 1st Order
36
Q

What are drugs that take part in the zero order elimination process?

A

High doses of

  • Ethanol
  • phenytoin
  • Salicylates (Aspirin)

PEA shaped like a O(Zero)

37
Q

Clearance =

A

Rate of drug elimination/Plasma concentration

Or Volume of distribution (Vd) X elimination constant ( Ke)

38
Q

Clearance formula in renal

A

Clearance = Free form x GFR

39
Q

Distinguish between the half life for zero order and first order

A

Half life is constant for First order elimination but it is not fixed for zero order elimination.

40
Q

What is the mathematical calculation of half life?

A

T1/2 = 0.7 x Vd/CL

41
Q

CSS is dependent on T1/2

True/false

A

True

42
Q

Difference between the mathematical steady state and clinical state

A

Mathematical steady state takes >7 t1/2 while clinical steady state takes >4 t1/2

43
Q

What is the formula of Css?

A

Css= Ro/CLt

Ro: the rate of infusion (does not change the time needed to reach CSS but it changes the concentration.

CLt: total clearance

44
Q

What is the mathematical calculation of Ro

A

Ro = Pc X CLt

Plasma concentration of the drug

45
Q

So is dosing rate same as rate of infusion ?

A

Yes

46
Q

What is the mathematical definition of maintenance dose

A

MD = Dosing rate X Dosing interval

Ro X DI

Or Cp X Cl X ^ /F

Pie(^) is dosing interval

47
Q

What is the calculation of loading dose?

A

LD = Vd X Css
Note if BV is less than 1 you should double the loading dose.

From FA—> LD = Cp X Vd / F(bioavailability)

48
Q

What are the characteristics of a drug receptor complex

A
  • Antagonism
  • Agonists
  • Efficacy
  • Potency
49
Q

What are the characteristics of a graded dose-response curve

A
  • Affinity
  • potency
  • Efficacy
  • Antagonism
50
Q

Affinity is

A

The ability to bind to the receptor

Closer to the y axis is more affinity

51
Q

Potency is

A

How much drug is required to produce a response

Determined by the affinity and the two drugs must have same efficacy

Represented by the. X-value

52
Q

Efficacy is

A

Maximum response provided by a drug

More efficient is the drug with the highest reached by the curve on y-axis

Increased y-value = increased Vmax

53
Q

In The presence of Agonist partial agonist acts as ?

A

A nonCompetitive antagonist as the efficacy is decreased but with independent potency decrease

54
Q

On the dose-response curves, competitive antagonists move agonist to where

A

A parallel shift to the right

It also decreases its potency

55
Q

Most antagonist are?

A

Competitive

56
Q

On the dose-response curves, non-competitive antagonists move agonist to where

A

A non-parallel shift to the right

It decreases both just efficiency and potency stays the same

57
Q

How many are the non-competitive drugs and what are they?

A

SPOD

  • succinylcholine CoA: nicotinic receptor
  • phenoxybenzamine: alpha receptors
  • organo phosphorus compound: AchE
  • Diazoxide:Alpha receptors
58
Q

What is pharmacological antagonism

A

An agonist and an antagonist competing for a single receptor and producing opposing effects

59
Q

Explain physiological antagonism

A

An agonist and an antagonist acting on different receptors but producing different opposing effects

60
Q

What is chemical antagonism?

A

The binding of a drug to another that the formation of complex between the effector drug and another compound reverses the action.

61
Q

What is the effective dose?

A

The amount of drug required to produce a response in 50% of test individuals

62
Q

What is a median toxic dose TD50

A

The amount of drug required to produce a toxic effect in 50% of test individuals

63
Q

What is a median lethal dose (LD50)

A

The amount of drug required to kill 50% of test individuals.

64
Q

What is therapeutic index

A

The relative safety of a drug

TI= LD/ED

OR

TI= TD/ED

65
Q

Drugs with very low therapeutic index

A
  • lithium
  • Warfarin
  • theophylline
  • digoxin
  • anti epileptic drugs

Warning these drugs are lethal

66
Q

What are the phases of drug testing

A

1- is it safe (safety and dosage on healthy humans)
2- does it work (efficacy and effectiveness)
3- is it better (safety, side effects,effectiveness)
4- can it stay (long term pros and cons post approval surveillance )

FDA approval occurs after phase 3

67
Q

What is the Micheal is menten kinetics?

A

It is Vi/o

=

[Vmax (S)] / [Km + (S)]

68
Q

In renal and liver dx ——- dose is decreased and _______ dose is unchanged

A

Maintenance dose

Loading dose

69
Q

Time to reach steady state depends on _____

A

T1/2 half life

And it is independent on dose and dosing frequency

70
Q

An increase in dose of drug leads to a ____ in the concentration of Cs

A

Increase

71
Q

More Pka mean

A

More basic

72
Q

Less Pka mean

A

More acidic

73
Q

Examples of competitive antagonist

A

Diazepam (agonist) + Flimazenil (antagonist) on GABA receptor

74
Q

Examples of non competitive antagonist

A

Norepinephrine (agonist) + phenoxybenzamine (antagonist) on alpha receptors

75
Q

Examples of partial competitive inhibitors

A

Morphine (full agonist) + buprenorphine (partial agonist) at opioid receptors

76
Q

Example of an addictive drug effect

A

Aspirin and acetaminophen

77
Q

Give an example of a permissive drug effect modification

A

Cortisol required for corticosteroids responsiveness

78
Q

An example of synergistic drug effect

A

Clopidogrel with Aspirin

79
Q

An example of potentiation drug effect modification

A

Carbidopa with no other therapeutic effect that to block the peripheral conversion of levodopa

80
Q

An example of antagonism drug effect

A

Ethanol antidote for methanol poisoning

81
Q

Drugs that exhibit tachyphylactic drug effect

A 
Hydralazine 
Niacin
Nitrate
Phenylephrine
LSD
MDMA

General Pharmacology (10 decks)

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