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CHEM358 Pharmacology > Pharmacodynamics- theory and checmicals > Flashcards

Pharmacodynamics- theory and checmicals Flashcards

1
Q

What is the action of competitive antagonists?

A

Competitive antagonists reversibly block receptors without activation and their effects are surmountable by increasing the dose of an agonist.

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2
Q

What is physiological antagonism?

A

Physiological antagonism occurs when two drugs produce opposing physiological effects via different biochemical pathways.

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3
Q

Selective Serotonin Reuptake Inhibitors (SSRIs) like fluoxetine are used to treat depression, and loop diuretics like furosemide are used for the treatment of oedema. These are examples of drugs inhibiting ???

A

are examples of drugs inhibiting transporters

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4
Q

For what conditions are Alpha 1-adrenoceptor agonists prescribed? Eg phenylephrine

A

Alpha 1-adrenoceptor agonists are used as nasal decongestants due to their vasoconstrictor effect.

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4
Q

Drugs like nitroglycerine and isosorbide dinitrate activate guanylate cyclase to relax vascular smooth muscle for angina relief. these are examples of drugs that ACTIVATE ???

A

examples of drugs that activate enzymes

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4
Q

Angiotensin II receptor blockers like losartan and β-adrenoceptor antagonists like propranolol are used to treat conditions such as high blood pressure and heart failure. These are examples of drugs inhibiting ???

A

examples of drugs inhibiting cell surface receptors

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5
Q

What are irreversible antagonists?

A

Irreversible antagonists have reactive chemical groups that form covalent linkages with receptors and their effects are not surmountable by increasing the dose of an agonist.

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6
Q

Kinase linked receptors, such as tyrosine kinase receptors, are activated following dimerization and their kinase domain is activated via ???

A

phosphorylation.

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7
Q

What is the use of enzyme activators? HINT: think of disease process driven by lack of …

A

Enzyme activators are used when the disease process is driven by too limited or lack of enzyme activity.

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8
Q

What determines a drug’s pharmacological activity? the combination of a drug’s ??? and distribution of its target receptor in cells and tissues

A

A combination of a drug’s specificity and the distribution of its target receptor in cells and tissues

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9
Q

What is the therapeutic use of GABAA chloride channel openers?

A

GABAA chloride channel openers like benzodiazepines are used for treating anxiety.

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10
Q

Cyclooxygenase inhibitors like aspirin and ACE inhibitors like captopril are used for pain relief and to treat high blood pressure, respectively. These are enzyme INHIBITORS or ACTIVATORS?

A

INHIBITORS

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11
Q

a medicine is a drug in a formulation that allows appropriate delivery. May involve improving:
* ???
* Stability
* Taste
* Physical form

A

Absorption

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11
Q

TRUE or FALSE: A drug is any substance or product that is used or intended to be used to modify or
explore physiological systems or pathological states for the benefit of the recipient

A

TRUE

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11
Q

drugs interact with biomolecules to exert chemical influence on ???

A

cellular function

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11
Q

Most drug targets are proteins such as
- Receptors, enzymes, carrier molecules (i.e. transporters) and ??? channels.

A

ion channels

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12
Q

TRUE or FALSE: drugs include endogenous substances such as hormones, neurotransmitters, ions, antibodies

A

TRUE

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13
Q

The interaction between drug molecules and drug targets impacts
??? function

A

physiological function

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14
Q

Agonists occupy receptors and activate or deactivate (?) cell processes

A

activate

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15
Q

A combination of a drug’s specificity
and the distribution of its target receptor in cells and tissues determines its ???

A

pharmacological activity

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16
Q

Antagonists occupy receptors but do not elicit a tissue response, hence also referred to as “inhibitors” as they inhibit a ??? response

A

physiological
response

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17
Q

Drug specificity refers to the relative
selectivity that a drug exhibits for a ???

A

receptor

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18
Q

Small changes in a drug’s chemical structure can cause loss OR gain (?) of activity because it no longer binds to its receptor. Alternatively, structure can also be manipulated to increase activity (whether agonistic or antagonistic)

A

loss only

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19
Q

TRUE or FALSE: No drug is completely specific for its target receptor

A

TRUE

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20
Q

Drug potency refers to the ??? of drug required to produce an effect

A

concentration

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20
Q

One drug is more potent than another if it acts on the same target (receptor) but elicits the same effect (i.e. EC50) at a lower OR higher (?) concentration

A

lower concentration

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20
Q

Drug affinity is a thermodynamic property reflecting the strength with which a drug binds to its target. Often measured as the equilibrium dissociation constant, ???

A

Kd

21
Q

Drug efficacy is the tendency of the drug to activate a tissue response once bound to its ???. Measured by differences in maximal response

A

receptor

22
Q

Competitive antagonists REVERSIBLY or IRREVERSIBLY (?) block receptors without activation. Effects surmountable by increasing agonist dose e.g. pseudoephedrine (adrenergic receptor agonist) vs propranolol (competitive adrenergic antagonist). Must have same receptor binding site

A

REVERSIBLY

23
Q

what type of antagonist has reactive chemical groups that form covalent linkages with receptors? HINT: Rarely used clinically, more useful in in vitro research

A

irreversible antagonists

24
Q

what type of antagonist doesn’t bind the same binding site on a receptor as the agonist?

A

non-competitive antagonists

25
Q

what type of antagonist binds an allosteric site causing a conformational change in the receptor that reduces the binding and response to an agonist AND effects are NOT surmountable?

A

non-competitive antagonists

26
Q

??? antagonism describes the binding of one drug to another, covalently or otherwise

A

chemical

27
Q

Antagonist effects the rate of absorption, excretion or metabolic degradation of another drug. what type of antagonism is this?

A

Pharmacokinetic Antagonism

28
Q

Histamine induces gastric acid secretion from parietal cells (stomach) whereas omeprazole blocks acid secretion by a totally different pathway - Omeprazole is a physiological antagonist of histamine. This is an example of what type of antaognism?

A

physiological antagonism

28
Q

Warfarin (anticoagulant) hepatic metabolism (inactivation) is accelerated by phenobarbital (induces liver enzymes), which reduces its anticoagulant effects. this is an example of what type of antagonism?

A

pharmacokinetic antagonism

29
Q

example of ion channels:
IP3 receptors
nicotinic acetylcholine receptors
P???

A

P2X receptors

29
Q

example of G-protein coupled receptors:
- P??? receptors

A

P2Y receptors

30
Q

7 transmembrane domaine G-protein coupled receptor and G protein interact at the interface of the membrane and ???

A

cytoplasm

31
Q

G-coupled protein receptors can be triggered by neurotransmitters which also activates ???

A

ligand-gated ion channels

32
Q

Kinase linked receptors (catalytic receptors): tyrosine kinase receptors are activated following ???

A

dimerisation

33
Q

Kinase linked receptors:
Kinase domain is activated via
???. Downstream signalling molecules signal via ??? reactions

A

phosphorylation

34
Q

examples of Kinase linked receptors (catalytic receptors):
- cytokine receptors
- integrins
- tyrosine ???

A

tyrosine kinase

35
Q

what type of receptors are typically activated by steroidal or non-steroidal hormones. Agonists diffuse across membrane (or via transporter). Bind to receptor in cytoplasm or nucleus and alter transcription in the nucleus (long-term changes)

A

nuclear receptors

36
Q

Drugs activating cell surface receptors:
Alpha 1-adrenoceptor agonists
constrict arterioles (vasoconstrictor)
e.g. phenylephrine, oxymetazoline
For use as nasal decongestants
agonist or antagonist?

A

agonist

37
Q

GABAA chloride channel openers for treating anxiety includes: benzodiazepines - Valium
This is an agonist or antagonist for ion channel opening?

A

agonist

37
Q

Potassium channel openers for vasodilation include: Minoxidil
This is an agonist or antagonist for ion channel opening?

A

agonist

38
Q

mu (μ)-opioid receptor agonists for
analgesia e.g. morphine. Endogenous ligand of μ-opioid receptor is endomorphin.
agonist or antagonist?

A

agonist

39
Q

Drugs activating nuclear receptors:
Oestrogen receptor agonists for hormone replacement therapy in post-menopausal women e.g. ???

A

estradiol

40
Q

what is an example of the drug molecule being the same structure as the native ligand? Hint: drug that activates nuclear receptors

A

estradiol

41
Q

Glucocorticoid receptor agonists for treatment of inflammation
* Hydrocortisone = endogenous
* Dexamethasone = non-endogenous
these agonists activate ??? receptors

A

activating nuclear receptors

42
Q

Activators of guanylate cyclase to relax
vascular smooth muscle for angina relief e.g. nitric oxide (NO)-generating organic nitrates
* Nitroglycerin
* Isosorbide dinitrate
agonists drugs that activate ???

A

enzymes

43
Q

Reactivators of cholinesterase after
poisoning with nerve agent or
organophosphate pesticides. e.g. ??? is an antidote which can cross
the BBB. An agonist that activates enzymes

A

Pralidoxime

44
Q

Calcium channel blockers for angina and high blood pressure
e.g. ???
Antagonist

A

Amlodipine

45
Q

Sodium channel blockers to prevent
propagation of nerve signals. e.g. ??? used as local anaesthetic
antagonist

A

Lidocaine

46
Q

Angiotensin II receptor (type1) blockers (AT1 antagonists) for treating high BP, heart failure, chronic renal insufficiency. e.g. ??? and ??? the sartans
(inhibit cell surface receptors)

A

losartan, valsartan

47
Q

β-Adrenoceptor antagonists for treating angina, myocardial infarction, high BP include: ???, metoprolol, atenolol
(inhibit cell surface receptors)

A

propanolol

48
Q

Mineralocorticoid receptor
antagonists for oedema due to liver
cirrhosis and heart failure. Is an aldosterone antagonist. (Drugs inhibiting nuclear receptors)

A

spironolactone

49
Q

Oestrogen receptor antagonists for the treatment of breast cancer. ??? can be used but efficacy is limited due to the risk of drug resistance
(Drugs inhibiting nuclear receptors)

A

tamoxifen

50
Q

Cyclooxygenase inhibitors inhibit
prostaglandin (inflammatory mediator) synthesis to provide pain relief. Known as non-steroidal anti-inflammatory drugs (NSAIDS).
e.g. ibuprofen, ???
(Drugs inhibiting enzymes)

A

aspirin

51
Q

Angiotensin Converting Enzyme (ACE) Inhibitors for high blood pressure, heart failure, and chronic renal insufficiency.
e.g. captopril, ???
(Drugs inhibiting enzymes)

A

ramipril

52
Q

Transporters bind to and shuttle membrane impermeable ligands across the cell membrane
e.g. ??? transporter, Serotonin transporter (SERT)

A

Noradrenaline

53
Q

TRUE or FALSE: Some drugs bind to transporters and cause changes that prevent proper functioning of transporters e.g. cocaine binding to noradrenaline transporter. Changes in the concentration of specific solutes (e.g. noradrenaline in synapses) mediate the effects of inhibitors of transporters.

A

TRUE

54
Q

Selective Serotonin Reuptake
Inhibitors (SSRIs) for the treatment of depression and anxiety are agonists inhibiting ???
e.g. Fluoxetine, paroxetine, citalopram

A

transporters

55
Q

Inhibitors of Na-2Cl-K symporter (loop diuretics) in renal epithelial cells to increase urine and sodium output for the treatment of oedema
e.g. ???, bumetanide
(Drugs inhibiting transporters)

A

Furosemide

56
Q

Drug potency refers to the ??? of drug required to produce an effect. One drug is more potent than another if it acts on the same
target (receptor) but elicits the same effect (i.e. EC50) at a lower
???

A

concentration
concentration

CHEM358 Pharmacology (11 decks)

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