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Phase 2 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Pharmacology:

ADME:

Factors affecting Absorption?

A

Absorption
Distribution
Metabolism
Excretion

Factors:
Bioavailability (AUC)
Gastric motility
pH partition/ionisation

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2
Q

Pharmacology:

Factors affecting Distribution?

A

Drug specific binding affects volume of distribution

Blood protein binding affinity for albumin for example

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3
Q

Pharmacology:

Factors affecting metabolism?

A

Enzyme induction e.g. Warfarin and Phenytoin - increased risk of bleeding Decreased INR

Enzyme inhibition e.g. Warfarin and Metronidazole - decreased metabolism of morphine increase
Increased INR

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4
Q

Pharmacology:

INR - what does it indicate

A

Indication of the time it takes for the blood to clot

Higher the INR = the longer it will take the blood to clot

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5
Q

Pharmacology:

Importance of grapefruit juice?

A

CYP3A4 inhibitor

Protein binding effects

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6
Q

Pharmacology:

Define
Druggability/ligandability
Efficacy

A

Druggability/ligandability - ability of protein target to bind drug/small molecule
Efficacy - ability of a drug to elicit its effect

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7
Q

Pharmacology:

Receptor activation steps

A

Binding of ligand
Conformational change within the protein
Causes action dependent on receptor
- signal transduction via secondary messengers (e.g. GPCR)
- Ligand-gated ion channel = opening of channel

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8
Q

Pharmacology:

Receptor classes

A

Ligand gated ion channels - Nicotinic Acetylcholine recptor
GPCRs - Beta-adrenoceptors
Kinase-linked receptors - Growth factor e.g. IGF receptor
Cytosolic/nuclear receptors - steroid receptors

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9
Q

Pharmacology:

Intrinsic activity definition?
Calculation?

A

Intrinsic activity – ability of a drug to produce a maximum functional response

Intrinsic Activity = Emax of partial agonist ÷ Emax of full agonist

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10
Q

Pharmacology:

Competitive inhibition?
Non-competitive inhibition?

A

Competitive inhibition = antagonist binds to the same site with higher affinity to

Non-competitive inhibition = Antagonist binds to allosteric binding site to reduce affinity of substrate

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11
Q

Pharmacology:

Cholinergic receptor subtypes:
Agonist and Antagonist for each? (not acetylcholine)

A

mAChR - muscarinic cholinergic receptor:
Agonist: Muscarinic
Antagonist: Atropine

nAChR - nicotinic cholinergic receptor:
Agonist: Nicotine
Antagonist: Curare

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12
Q

Pharmacology:

Irreversible antagonist? 
Receptor reserve?
Allosteric modulation? 
Inverse Agonist? 
Tolerance?
Desensitisation?
A

Irreversible antagonist: covalent bonding inactivation
Receptor reserve: agonist only requires small fraction of receptors to elicit maximal reponse
Allosteric modulation: binding at site other than active site modulates receptor affinity for ligands
Inverse agonist: binding produces opposite response
Tolerance: reduction in agonistic effect due to repeated stimulation
Desensitisation: result of tolerance, receptor uncoupling, degradation and internalisation

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13
Q

Pharmacology:

Enzymes as drug targets:
Statins?
ACEi?
Parkinson’s treatment?

A

Statins: HMG co reductase - rate limiting step in cholesterol synthesis
e.g. Atorvastatin

ACEi: angiotensin converting enzyme inhibition (RAAS manipulation)
e.g. enalapril

Parkinson’s treatment: Target MAO (monoamine oxidase) to prevent dopamine degradation
COMT/DDC inhibition prevent L-DOPA degradation

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14
Q

Pharmacology:

Transporters as targets: 
Diuretics: ENaC? NKCC?
Ca channel blocker? 
Na Channel blocker? 
Cl- Channel poteniator?
A

ENaC - Thiazide diuretics
Na K Cl symporter - Furosemide (loop diuretic)
Ca antagonist: Amlodipine
Na antagonist: Lidocaine
Cl- modulator: Benzodiazepines increase Cl-

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15
Q

Pharmacology:

Pumps as targets:
Na/K ATPase
K/H ATPase proton pump

A

Na/K ATPase - Digoxin

PPI - Omeprazole (irreversible antagonism)

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16
Q

Pharmacology:

Routes of administration:
Intrathecal?
Intra-articular?
Intravitreal?

A

Intrathecal – through the theca of the spinal sheath into the subarachnoid space

Intra-articular – injection into a joint capsule e.g. knee in arthritis

Intravitreal – into the eye (vitreous fluid) e.g. Avastin in wet macula degeneration

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17
Q

Pharmacology:

Passage across membranes:? (5)
Example for each?

A 
Diffusion - Ion channel
Passive diffusion - Steroids
Active transport - P-gp (drug remover transporter)
Pinocytosis 
Facilitated diffusion - glucose
18
Q

Pharmacology:

Passive diffusion = water or lipid/fat soluble?

Facilitated diffusion = water or lipid/fat soluble?

A

Passive diffusion molecule must be lipid soluble

Facilitated diffusion molecule must be small and water soluble

19
Q

Pharmacology:

Drug ionisation: Dependent on what?

Which form is water soluble/fat soluble?

A
  • Strength of ionisable group
  • pH of solution drug is in
    PKa

Ionised form = water soluble
Unionised form = lipid soluble

20
Q

Pharmacology:

Best absorption for weak acids and bases?

A

Weak acid = Stomach as low pH so less of the drug will be ionised form

Weak base = intestine higher pH so less drug will be ionised form

21
Q

Pharmacology:

Enteric coating?
Modified release tablets?

A

Enteric coating: protection against low pH

Modified release tablets: slow release

22
Q

Pharmacology:

Parasympathetic Nervous System which Rest/Flight?
Short/long pre? 
Short/long post? 
Nerve transmitters? 
Receptors? 
Sympathetic Nervous System which Rest/Flight? 
Short/long pre? 
Short/long post?
Nerve transmitters? 
Receptors?
A

Parasympathetic: Rest and Digest

  • Long preganglionic
  • Short postganglionic
  • ACh at every step
  • Pre = nicotinic AChRs
  • Post = muscarinic AChRs

Sympathetic: Fight or flight

  • Short preganglionic
  • Long postganglionic
  • ACh pre then Adrenergic (NA/AD)
  • Pre = nAChRs
  • Post = Alpha/Beta and ACh (sweat glands only) adrenergic receptors
23
Q

Pharmacology:

Dopamine is a precursor to what?

A

Dopamine –> Noradrenaline –> Adrenaline

24
Q

Pharmacology:

Adrenergic receptor subtypes and their effects:
Alpha adrenoceptors?
Beta adrenoceptors?

A

Alpha 1 + 2 (smooth muscle so BP) Alpha 1 contracts

Beta 1 - chronotropic and inotropic effects
Beta 2 - bronchodilation, vasodilation: relaxation of smooth muscle
Beta 3 - bladder

25
Q

Pharmacology:

Hypersensitivity: Gel and Kumes classification
Type 1-4?
Example for each?

A

Type 1: IgE + mast cell mediated - degranulation e.g. acute anaphylaxis
Type 2: Antibody dependent cellular cytotoxicity e.g. transfusion reactions/autoimmune
Type 3: Immune complex and activation of complement e.g. SLE, farmers/pigeon fanciers lung
Type 4: T-cell mediated e.g. TB (granulomas)

26
Q

Pharmacology:

ADRs
Rawlins classification? ABCDEF

DOTS

A 
A= Augmented 
B= bizarre/idiosyncratic
C= Chronic/continuous
D= delayed
E= end of treatment (withdrawal) 
F= failure of therapy

DoTS - Dose related, Timing, susceptibilty

27
Q

Pharmacology:

Anaphylaxis due to drugs:
Features of anaphylaxis?

A
  • Vasodilation (flushing) Anaphylactic shock
  • Increased vascular permeability (oedema)
  • Bronchoconstriction
    Wheezing/SOB Cyanosis
  • Urticaria (rash)
  • Angio-oedema (swelling of face/throat)
28
Q

Pharmacology:

ADRs can be any of the 4 types of hypersensitivity

A

Type 1: Anaphylaxis
Type 2: Drug/metabolite combine with protein
Type 3: form immune complexes
Type 4: contact dermatitis

29
Q

Pharmacology:

Non-immune anaphylaxis?

A

no prior exposure; allergen has innate ability to activate mast cells

30
Q

Pharmacology:

Treatment of anaphylaxis?

A

Adrenaline
Antihistamines
Steroids
Basic life support

31
Q

Pharmacology:

PKa - Dissociation constant

A

pH at which half of the substance is ionised and half is unionised

32
Q

Pharmacology:

Routes of membrane passage? (4)

A

Passive diffusion - steroids
Diffusion through pores/ion channels - lithium
Carrier mediated transport e.g. OAT1, P-gp
Pinocytosis (Amphotericin)

33
Q

Pharmacology:

Factors affecting oral absorption? (4)

A

Drug structure (solubility/stability at pH)
Formulation
Gastric emptying
First pass metabolism (Intestinal lumen/wall, liver, lungs)

34
Q

Pharmacology:

Phase 1 vs Phase 2 metabolism

A

Phase 1:
Degradative
Intro of functional group
Increases polarity

Phase 2:
Conjugative
Increases hydrophilicity

35
Q

Pharmacology:

First order kinetics?

Zero order kinetics?

A

A constant amount of the drug is eliminated per unit time

If an enzyme stystem that removes a drug is saturated the rate of removal of a the drug is constant and unaffected by increased drug concentration

36
Q

Pharmacology:

Bioavailibility (F) = ?
Bioavailibility of 0.1 what does the oral dose need to be compared to the i.v. dose?

A

AUC oral / AUC iv

AUC iv is 100%

10x higher as oral AUC is 10% of I.V.

37
Q

Pharmacology:

Water soluble drugs’ distribution depends on?
Lipid soluble drugs’ distribution depends on?

A

water soluble = rate of passage across membranes

lipid soluble = rate of blood flow to the tissue

38
Q

Pharmacology:

Vd - apparent volume of distribution
What does low/high mean?

A 
Vd = total amount of drug in the body (dose) / plasma concentration
Low = confined to bloof 
High = distributed in body water
39
Q

Pharmacology:

Clearance (CL)

A

Volume of drug cleared(excreted) per unit time
CL=Dose/AUC for i.v.
CL=Dose/(FxAUC) for oral

40
Q

Pharmacology:

Steady state (Css)
For I.V. ?
For Oral?

A

I.v.: Css = rate of infusion/ CL

Oral: Css = D x F/ t x CL

Phase 2 (4 decks)

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