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Year 2 - LCRS > Pharmacology - Autumn > Flashcards

Pharmacology - Autumn Flashcards

1
Q

Where are the different types of muscarinic receptors located?

A

M1 - Neural (memory and Learning) (Gq) M2 - Cardiac (Gi) M3- Exocrine and Smooth muscle (Gq)

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2
Q

Nicotinic and muscarinic. Which is g protein linked and which is ionotropic

A

Nicotinic - Inotropic FAST Muscarininc - G Protein linked - SLOW

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3
Q

What is special about the autonomic control of arterioles?

A

No parasympathetic control

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4
Q

Describe the synthesis of Acetylcholine

A

AcetylCoA + Choline (Choline Acetyltransferase CAT) =Ach + CoA

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5
Q

Describe the breakdown of Ach

A

Ach (acetylcholinesterase) Choline + Acetate

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6
Q

Describe the synthesis of Noradrenaline

A

Tyrosine (tyrosine hydroxylase) Dopa (Dopa decarboxylase ) dopamine (Dopa beta Hydroxylase) Noradranline

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7
Q

How is noradrenaline broken down ?

A

Uptake 1 = Monoamine Oxidase A (MAO-A) Uptake 2 = COMT

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8
Q

Differentiate between pharmacokinetics and pharmacodynamics

A

Pharmacokinetics = effect of the body on the drug Pharmacodynamics = Effect of the drug on the body

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9
Q

Outline what is meant by non-specific drug action

A

Produce responses to physiochemical properties e.g. Antacids - basic compound neutralises stomach acid

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10
Q

What is AFFINITY

A

How willingly a drug binds to a receptor

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11
Q

EFFICACY

A

the ability of a drug to generate a response

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12
Q

Describe the change in a dose-response curve between an agonist and a second agonist of lower affinity.

A

Curve moves to the right

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13
Q

Describe the change in a dose-response curve between an agonist and a second partial agonist

A

Same starting point but only reaches half tissue response Ss

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14
Q

Why does claryrhromycin potentiate warfarin?

A

They are metabolised by the same pathway

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15
Q

What is INR

A

International Normalised ratio -prothrombin time ~10secs so physiological INR should be 1

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16
Q

Name another drug class that is an inducer of the liver enzymes for warfarin

A

Barbiturates

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17
Q

What is the mechanism of action of digoxin?

A

Blocks the K+ binding site on the external K+/Na+ ATPase

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18
Q

Why might digoxin dosage need to be less for older patients?

A

Liver/kidney function declines with age. (Digoxin primarily cleared by the kidney) so would be cleared more slowly.

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19
Q

Why might malnutrition affect the efficacy of warfarin

A

warfarin is 90% plasma bound. If malnourished there is a decrease in plasma protein. Heavily bound drugs are very sensitive to changes in plasma protein levels.

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20
Q

What are the 4 types of ion channels that control contraction of the heart muscle?

A

If = funny channel (Na Channel) Ca(t)= Transient. Opens first Ca(l)= Long lasting. K channels repolarisation.

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21
Q

Name 3 organs that are largely under parasympathetic control

A

Lungs, Eyes, Heart (at rest)

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22
Q

What effect does the the following receptors have on the vasculature? Alpha 1 adrenoreceptor Beta 2 adrenoreceptor

A

Alpha 1 adrenoreceptor - constricts Beta 2 adrenoreceptor - dilates

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23
Q

Out of the 4 types of receptors how many are membrane bound and which if any is not ?

A

3 are membrane bound. Only Type 4 (Intracellular steroid type receptors) are intracellular

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24
Q

Name a cardiac glycoside and outline its mechanism of action

A

Digoxin - Binds the K+ binding site of the K+/Na+ pump. Slows down the exchange therefore increasing the intracellular Ca2+ and increases contractility. = inc. contractility of the heart

25
Q

Give an example of a competitive antagonist

A

Atropine -Competitive muscarinic cholinoceptor antagonist

26
Q

Explain enterohepatic cycling

A

The drug or metabolites get excreted into the gut from the liver. But they are reabsorbed and returned to the liver via enterohepatic circulation. Can lead to drug persistence

27
Q

What is bioavailability

A

The proportion of a drug that is available within the body to exert its pharmacological effect (after it leaves the liver and enter the systemic circulation)

28
Q

Explain first order kinetics

A

elimitation of a drug is at a rate that is proportional to the concentration of a drug remaining in the body. (Log concentration vs time = straight line )

29
Q

Explain zero order kinetics and give an example of a drug cleared this way

A

A constant amount of drug is cleared per unit of time (eg alcohol) (Concn vs time = straight line)

30
Q

List 5 mechanisms of drug tolerance

A
  1. Pharmacokinetic factors - Metabolism increases
  2. Loss of Receptors - membrane endocytosis
  3. Change in receptors - Conformational change
  4. Exhaustion of mediator stores - eg amphetamines
  5. Physiological adaptation - “homeostatic response”
31
Q

What does parenteral mean

A

Everything but the GI tract

32
Q

How would you describe the shape of a log dose-response curve?

A

Sigmoid

33
Q

What are the 2 ways a drug moves around the body ?

A

Bulf flow transfer (as a bolus)

Diffusional transfer (molecules diffusing)

34
Q

In which part of the kidney are lipid soluble drugs reabsorbed?

A

In the proximal and distal tubules

35
Q

What are the 3 types of Phase 1 metabolism reactions?

A

Oxidation (mainly this for phase 1)

Reduction

Hydrolysis

36
Q

What is the primary purpose of Phase 1 Reactions?

A

Introduce an accessible functional group into the molecule

37
Q

What is the primary purpose of Phase 2 meabolic reactions

A

Adds a large polar endogenous molecule - allows excretion

38
Q

What group do CYP450 enzymes have at the active site?

A

A porphyrin ring and (Fe3+) iron

39
Q

What 4 factors influence drug distribution:

A
  • Regional blood flow
  • Extracellular binding (plasma protein binding)
  • Capillary permeability
  • Localisation in tissues
40
Q

Where does active secretion of a acids and bases take place?

A

In the proximal tubule

41
Q

Which three products are generated by a CYP 450 reaction

A

NADP+
oxidised drug

water

42
Q

List 4 common Phase 1 oxidative metabolism reactions

A

Hydroxylation
N-demethylation
O-demethylation
N-oxidation (not a CYP450 reaction)

43
Q

Which enzyme catalyses N-oxidation

A

Flavin Containing Monooxygenase (FMO)

44
Q

What is the cause of fish odour syndrome

A

Deficiencey of Flavin Containing Monooxygenase (FMO3) so can’t metabolise trimethylamine so excrete it in sweat and breath.

45
Q

What catalyses hydrolysis reactions?

A

Esterases

Amidases

46
Q

What are the characteristics of the products of Phase 2 metabolism reactions?

A

The conjugate that is formed is almost always inactive

It is less lipid soluble

It is more polar

It is easier to excrete

47
Q

What are the 6 Phase 2 metabolism reactions?

A
  • *G**lucoronidation - Most common
  • *A**cetylation
  • *M**ethylation
  • *S**ulphation
  • *A**minoacid conjugation
  • *G**lutathione conjugation
48
Q

Glucoronidation - What is it? What is the conjugating agent ? The catalyst? and what properties do the compounds generated have?

A

Glucoronidation = The addition of a sugar to a foreign compound
Catalyst = glucuronyl transferase
Conjugating agent = UDPGA

Products are polar and often high molecular weight

49
Q

Very basically outline the properties of the andrenergic receptors

A

alpha1- Vasoconstriction
Alpha2- presynaptic negative feedback
B1- Tachycardia
B2 - Relaxation of smooth muscle(_Bronchodilatio, uterine smooth muscle relaxation in threatened pre-term labour) (suppress inflammatory mediators)

50
Q

Give two examples of directly acting cholinomimetic drugs

A

1) Choline esters (bethanechol)
2) Alkaloids (pilocarpine)
Both drugs have very similar structures to acetylcholine

51
Q

What is pilocarpine? What are it’s main uses and side effects?

A

A non-selective muscarinic agonist with good lipid solubility. Particularly useful in ophthalmology as a local treatment for glaucoma
Side effects: blurred vision, sweating, gastrointestinal disturbance and pain, hypotension, respiratory distress

52
Q

What is bethanechol? What are it’s main uses and side effects?

A

A selective M3 acetylcholine receptor agonist. Mainly used to assist bladder emptying and to enhance gastric motility.
Side effects: sweating, impaired vision, nausea, bradycardia, hypotension, respiratory difficulty

53
Q

What anticholinesterase drugs are used to treat Alzheimer’s disease?

A

Donepezil

Rivastigmine

Galantamine

Memantine (NMDA receprtor blobcker)

54
Q

Why are excipients added to a drug formulation?

A

To alter bioavailability of a drug
To improve the flavour of the drug
To reduce the rate at which the drug is released into the blood

55
Q

Give two examples of nicotinic receptor antagonists.

A

Hexamethonium
Trimetaphan

56
Q

Give examples of muscarinic receptor antagonists. (3)

A

Atropine
Hyoscine
Tropicamide

57
Q

Give examples of directly acting SNS agonists and the receptor they selectively bind?

A

Adrenaline (non-selective)
Phenylephrine (α1)
Clonidine (α2)
Dobutamine (β1)
Salbutamol (β2)
Higher concentrations of drugs will start to lose selectivity and effect other receptors

58
Q

When does ingestion of tyramine cause problems?

A

When taking MAO inhibitors tyramine competes with MAO which is required for the breakdown of NA
Causes hypertensive crisis

59
Q
A

Year 2 - LCRS (9 decks)

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