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MD1 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

5-Lipoxygenase

A

Converts Arachidonic Acid to Leukotrienes

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2
Q

ACE Inhibitors

A 
Angiotensin Converting Enzyme Inhibitors
Block angiotensin I -> angiotensin II
'prils'
Reduces blood volume and vascular tension (affects of Angiotensin II)
Inhibits breakdown of Bradykinin

Contraindicated in pregnancy (teratogenic)

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3
Q

Acetylcholine

  • effects
  • production
A

Neurotransmitter (ANS - CNS & PNS)
Only neurotransmitter used in the motor division of the somatic nervous system. Acetylcholine is also the principal neurotransmitter in all autonomic ganglia.

Has inhibitory effect in cardiac tissue (lower HR)
Excitatory neurotransmitter at neuromuscular junctions in skeletal muscle. Causes smooth muscle contraction at high concentrations

Choline + AcetylCoA = Acetylcholine + CoA

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4
Q

Adrenaline, noradrenaline

  • receptor
  • production

(epinephrine, norepinephrine)

A

α and β-adrenoceptor agonist
Catecholamines

NA Synthesis
Tyrosine –(Tyrisoine Hydroxylase)–> L-DOPA –(DOPA decarboxylase)–> Dopamine –(Dopamine beta-hydroxylase)–> Noradrenaline

Adrenaline Synthesis
(as before) Noradrenaline –(Phenylethanolamine-N-methyl transferase)–> Adrenaline

Broken down by MAO (mono-amine oxidase)

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5
Q

Alteplase

A

Fibrinolytic, activates plasminogen (to plasmin)
Clot Selective, Very Expensive
Short Half Life (IV infusion)

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6
Q

Aminoglycosides

A

MECHANISM:
Bind to ribosome and distort reading frame (bacteria makes abnormal proteins) - leads to faulty cell wall.
Total protein synthesis block

BACTERIA:
GNRs
E coli
Klebsiella
Pseudomonas

NAMES:
Gentamicin
Tobramicin
Streptomycin (TB)

SIDES:
Hearing Loss
Vertigo
Kidney Damage

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7
Q

Amiodarone

A

K+ Channel Inhibitor
Prolong cardiac action potential
Amiodarone also blocks Na+, Ca+, and β-adrenoceptors
Adverse effects:
reversible photosensitisation, skin discolouration, and hypothyroidism
Causes pulmonary fibrosis with long term use

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8
Q

Ampicillin

A

Beta-lactam
GPC, GPR, GNC, GNR
Broad spectrum - binds many penicillin binding proteins and very soluble
Pseudomonas auriginosa are intrinsically resistant because they have a chromosomally encoded beta-lactamase

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9
Q

Amrinone

A 
Phosphodiesterase 3 Inhibitor
Increase cAMP
Increase Protein Kinase A (PKA) activity
Increase intracellular Ca2+
Increase contractility
(also causes vasodilation - cGMP)
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10
Q

Angiotensin Receptor Antagonists

A

‘sartans’

vasodilation
reduced blood pressure
Reduce aldosterone
Reduce cardiac hypertrophy
Reduce sympathetic activity
Adverse effects:
hyperkalaemia
headache, dizziness
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11
Q

Aspirin

A

Acetylation of COX (inhibitor)

  • anti-inflammatory
  • Aspirin Triggered Lipoxins - resolution of inflammation
  • analgesic
  • anti-pyretic
  • anti-coagulant (low dose 80mg)
  • contraindicated in gout (competes with uric acid in kidney for excretion)
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12
Q

Astemizole

A

H1 Receptor Antagonist (Competitive / Reversible)
Non sedative
Lack anti-muscarinic activity and GIT effects

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13
Q

Atenolol

A

β1adrenoceptor antagonist (decrease HR & Contractility)

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14
Q

Atropine

A

Anti-muscarinic (competitive antagonist at parasympathetic AChR)
Reduce secretions (e.g. Salivation)
Bronchodilator (in anaesthesia)
Treatment of bradycardia (block M2, parasympathetic)
Increase HR
Pupil dilation
AChE-inhibitor poisoning

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15
Q

b-lactams

A

Inhibit bacterial cell wall synthesis

Include penicillins

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16
Q

Botulinum Toxin

A

Prevents SNARE proteins from binding thereby preventing synaptic vesicle from releasing neurotransmitters

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17
Q

Bradykinin

A

Autacoid
Prekallikrein -(hageman/Factor XII)-> kallikrein -> HMWK -> bradykinin
Degraded by ACE
Stimulate Release of PGI2 and NO (Vasodilation)
Stimulate sensory nerve endings (Pain)
Contract uterus, airways, gut (smooth muscle)
Epithelial secretion in airways, gut

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18
Q

Ca2+ Channel Blocker

A

Cardioselective blockers (Verapamil) most effective at SA and AV nodes, reduce rate and conduction
Adverse effects:
Facial flushing, peripheral oedema, dizziness, bradycardia, headache, nausea

Verapamil
Diltiazem (also vasodilator)
Nifedipine

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19
Q

Captopril, Enalapril, Perindopril, Ramipril

A 
ACE Inhibitors (block angI -> angII)
Reduce vascular tone (vasodilation)
Reduce Aldosterone production
Reduce Cardiac Hypertrophy
Prevent Bradykinin breakdown
Adverse Effects:
First-dose hypotension
Dry cough
loss of taste
hyperkalaemia
acute renal failure
itching, rash, angio-oedema
foetal malformations
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20
Q

Carbenicillin

A

GNR (Pseudomonas Aeruginosa)

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21
Q

Cetirizine

A

H1 Receptor Antagonist (Competitive / Reversible)

Reduced risk of unwanted cardiac effects

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22
Q

Chlopheniramine

A

H1 Receptor Antagonist (Competitive / Reversible)

Sedative

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23
Q

Cholestyramine, colestipol

A

Bind bile acids (cholesterol metabolites) preventing gut absorbtion
Upregulation of hepatic LDL receptors (to synthesize bile acids)
Removal of LDL from plasma and increased cholesterol metabolism

ADVERSE EFFECTS:
abdominal discomfort, bloating, constipation, flatulence
rare: increased triglycerides, fecal impactions, decreased fat soluble vitamin absorbtion, fatty stool (steatthorea)
Decreased drug absorbtion (thiazides, aspirin, glucosides) - give drugs before resins

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24
Q

Cisplatin

A 
Cytotoxic anticancer agent (prostate tumors)
Causes nephrotoxicity (blood & protein in urea, kidney damage)
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25
Q

Clavulanic Acid

A

Suicide inhibitor of β-lactamase
Doesn’t inhibit chromosomally encoded resistances
combine with amoxycillin (β-lactam)

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26
Q

Clopidogrel

A

ADP receptor antagonist
Inhibits platelet activation and adhesion
Oral prodrug

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27
Q

Cocaine

A

Block reuptake of Noradrenaline from synapse
(similar for dopamine and serotonin)
Produce tachycardic effect and heightened Blood Pressure, dysrhythmia

Also blocks Na+ channels - precursor for local anaesthetic drugs

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28
Q

COX

A

Cyclooxygenase
Catalyses Arachidonic Acid -> PGE2, PGD2, PGF2
COX1 - constitutive, COX2 - inducible (IL-1)

COX2 expressed in vessel wall by steady laminar shear stress

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29
Q

Digoxin

A

Glycoside
Decrease HR (increase vagal activity)
Increase contractility
- Inhibit Na+/K+-ATPase, increasing intracellular Ca2+
- Decrease Ca2+ in sarcoplasmic reticulum
Affects Gut, CNS, Cardiac

Forms complex with Aromatic hydrocarbon receptor nuclear translocator which increases P450 gene expresion

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30
Q

Dobutamine

A

β1 adrenoceptor agonist (increase HR & Contractility)

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31
Q

Donepezil

A

Anticholinesterase (acetylcholinesterase inhibitor)
Prevents breakdown of ACh
Enters CNS well
Treatment of Alzheimers

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32
Q

EC50

A

concentration of a compound where 50% of its maximal effect is observed

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33
Q

ED50

A

effective dose, for 50% of people receiving the drug

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34
Q

Edrophonium

A

Anticholinesterase
Short duration
Diagnosis of myasthenia gravis

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35
Q

Endothelin

A

Vasoconstrictor

produced by vascular endothelium

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36
Q

Ezetimbe

A

Inhibits cholesterol absorbtion in intestine by binding to sterol transporter
Does not affect absorbtion of bile acids or fat soluble vitamins
lowers LDL
ADVERSE EFFECTS:
diarrhoea, headache, tiredness
allergic reaction, severe joint or stomach pain

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37
Q

Flecainide

A

Class 1c Na+ Channel Blocker
Marked Na block
Same repolarisation
No effect on ERP

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38
Q

Flucloxicillin

A

GPC (Staphylococcus)

beta-lactam with narrow-spectrum

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39
Q

Furosemide / Frusemide

A 
Loop Diuretic (loop of henle)
inhibit Na+/K+/2Cl- carrier into cells
Well absorbed (<1hr)
Duration (3-6 hours)
Adverse effects:
hypokalaemia
metabolic alkalosis
hypovolaemia and hypotension
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40
Q

Gemfibrozil, fenofibrate

A

Fibrates - lower lipid levels
Agonist at nuclear receptor (regulate gene expression)
peroxisome proliferator activated receptor alpha agonist
increased synthesis of liproprotein lipase (LPL)
increased lipolysis of lipoprotein TG
reduction in plasma TGs
increase in HDL
variable effect on LFL

ADVERSE EFFECTS:
elevation of serum aminotransferase
nausea, dry mouth, headache, rash
rare: arrhythmias, gallstones, photosensitivity, impotence, depression

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41
Q

Gentamicin

A

Aminoglycoside

High toxicity (renal elimination damages kidney and impares excretion)

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42
Q

Glycopeptides

A

MECHANISM:
Target bacterial cell wall (inhibit peptidoglycan synthesis)

BACTERIA:
GPs (including MRSA)
C difficle

NAMES:
Vancomycin

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43
Q

Glycosides

A

Gut - anorexia, nausea, diarrhoea
CNS - drowsiness, confusion, psychosis
Cardiac - ventricular dysrhythmias
see digoxin

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44
Q

Heparin

A

Anticoagulant
Enhance activity of anti-thrombin III which inhibits IIa (Thrombin) IXa, Xa, XIa, XIIa
Given via IV (large & negative charged molecule)

Measured by APTT (activated partial thromboplastin time) - time it takes for blood to clot

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45
Q

Hexamethonium

A

Ganglion Blocker

Nicotinic AChR antagonist

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46
Q

Histamine

A 
H1:
Vasodilation, 
Vascular Permeability
Bronchoconstriction
Smooth muscle contraction
\+
Pain & itch (sensory nerve activation)
Mucous secretion
CNS - increased wakefulness

H2:
Gastric acid secretion
Positive inotropic and chronotropic effects

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47
Q

Hydrochorothiazide

A

Thiazide Diuretic
inhibity Na+/Cl- cotransporter in distal convoluted tubule
lower blood volume and reduce BP
Adverse effects:
K+ loss, gout, hyperglycaemia, allergic reaction

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48
Q

Ipratropium Bromide

A 
Treatment of COPD
Anti-muscarinic (non selective)
blocks muscarinic (M3) AChR in smooth muscle of bronchi
Tiotropium Bromide (LAMA), M3 selective.
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49
Q

Isoprenaline

A

β1& β2 adrenoceptor agonist

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50
Q

K+ Channel Block

A

Delay phase 3 of ventricular action potential (K+ efflux)
Decrease incidence of re-entry
Increase risk of triggered events

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51
Q

Lignocaine

A

Class 1b Na+ Channel Blocker
Mild Na block
Decrease ERP

Local Anaesthetic (aminoamide) - prevent action potention transmission
Long acting, hepatic metabolism
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52
Q

Loop Diuretics

A 
Act on thick ascending limb of loop of henle
inhibit Na+/K+/2Cl- carrier into cells
Well absorbed (<1hr)
Duration (3-6 hours)
Adverse effects:
hypokalaemia
metabolic alkalosis
hypovolaemia and hypotension
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53
Q

Loratidine

A

H1 Receptor Antagonist (Competitive / Reversible)

Reduced risk of unwanted cardiac effects

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54
Q

Losartan, Candesartan

A 
Angiotensin Receptor (AT1/AT2) Antagonist
Reduce vasoconstriction
Reduce aldosterone
Reduce cardiac hypertrophy
Reduce sympathetic activity
Adverse effects:
hyperkalaemia
headache, dizziness
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55
Q

LTB4

A

Leukotriene B4

Promotes Inflammation by attracting leukocytes

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56
Q

LTC4, LTD4, LTE4

A 
Leukotreines
Bronchoconstrictors
Vasoactive
Vessel permeability
Increased mucous production
Asthma (w/ aspirin)
Inhibited by Montelukast
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57
Q

MAOI

A

Monoamine Oxidase Inhibitor

prevent breakdown of Noradrenaline, increasing rate of secretion and synaptic concentration

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58
Q

Methicillin

A

GPC (Staphylococcus)

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59
Q

Metronidazole

A

Avtivated by strict anaerobe reducing enzymes (used to keep environment free of oxygen)

Also good for trichnomoniasis, amoebiasis, and giardiasis

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60
Q

Muscarinic AChR

A 
G-Protein Coupled Receptor
Autonomic NS
Salavation, Lactimation, Urination, Defecation
Sweating
Decrease HR
Bronchoconstriction
Vasodilation
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61
Q

Na+ Channel Block

A

Reduce phase 0 slope and peak of ventricular action potential (depolarization involving Na+ influx)

Quinidine 1a
Lignocaine 1b
Flecainide 1c

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62
Q

Neostigmine, Pyridostigmine

A

Anticholinesterase
Reverse effect of non-depolarising neuromuscular blockers
Treatment of myasthenia gravis (LMNL)

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63
Q

Niacin / Nicotinic Acid

A

For treatment of hypercholesterolaemia (mechanism unclear)
decrease VLDL secretion
reduction in plasma LDL and TG
increase in HDL
decrease lipoprotein(a) - formed from LDL in plaques and inhibits thrombolysis

ADVERSE EFFECTS:
Vasodilation, flushing, hypotension
Nausea, vomiting
Tolerance
Rare: itching, glucose intolerance, uric acid retention, hepatic imparement
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64
Q

Nicotinic AChR

A

Ligand Gated Ion Channel
Somatic NS / Autonomic NS
Skeletal (Somatic) muscle contraction

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65
Q

Nitrates

A 
Venodilators (primarily)
Some vasodilation
Treatment of Angina 
1st pass metabolism
increased tolerance (and sensitivity to constrictors)
Reduce preload & cardiac work

release NO -> stimulates guanylate cyclase in smooth muscle -> GTP converted to cGMP-> myosin LC-PO4 dephosphorylated to myosin LC -> vascular relaxation

ADVERSE EFFECTS:
relaxation of gut, airway smooth msucle
postural hypotension (venous pooling)
headache, flushing
reflex tachycardia (usually given in combination with beta-blocker to minimize)
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66
Q

Nitric Oxide (NO)

A

Vasodilator
Inhibit platelet adhesion and aggregation
Also known as Endothelium Derived Relaxant Factor
Increased intracellular Ca2+ catalyses NOS inactive to NOS active which catalyses arginine to NO + citrulline
NO catalyses pathway causing cGMP production (relaxation). cGMP is degraded to GMP (can be blocked by Viagra)

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67
Q

NSAID

A

Inhibit COX

  • anti-inflammatory
  • analgesic
  • anti-pyretic (reduce fever)
  • anti-coagulant

SIDES:

  • increased bleeding time (decrease TXA2)
  • GI (reduced mucous, increased acid, reduced blood flow and angiogenesis)
  • reduced renal blood flow (decreased PGI dilation)
  • triple whammy
  • bronchoconstriction (overproduction of leukotrienes)
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68
Q

Osmotic Diuretics

A 
pharmacologically inert (e.g. mannitol sugar molecule)
reduce passive water reabsorbtion
use in raised intercranial/interocular pressure
prevent acute renal failure
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69
Q

Penicillin G

A

GPC, GPR, GNC

Bacteriostatic (bacteria detect cell wall defect and break down their own wall)

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70
Q

Penicillin V

A

GPC, GPR, GNC

less effective than penicillin G against Gram negatives

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71
Q

PGD2

A

Bronchoconstrictor

Does not circulate

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72
Q

PGE2

A 
Vasodilator (decrease BP)
Angiogenic (healing)
Pyrogenic (fever)
Hyperalgesic (pain)
Increase mucous secretion
Decrease gastric acid secretion
Does not circulate
Induction of labour & abortant
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73
Q

PGF2

A

Bronchoconstrictor

Does not circulate

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74
Q

PGI2

A 
Prostacyclin
Vasodilation,
Inhibits platelet aggregation/activation
Anticoagulant
Secreted by vascular endothelium
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75
Q

Phenylephrine

A

α1 adrenoceptor agonist (vasoconstrictor)

useful as nasal decongestant

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76
Q

Phospholipase A2

A

Releases Arachidonic Acid from Cell Membrane

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77
Q

Pilocarpine

A

Reduce interocular pressure (glaucoma)

Autonomic NS Muscarinic AChR agonist

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78
Q

Polyenes

- amphotericin B

A

Antimicrobial targets fungi
Attacks ergosterol in cytoplasmic membrane (very toxic - also attack cholesterol)
Cause K+ and Na+ leakage -> cell death

allylamines, triazoles (fluconazole), morpholines affect synthesis of ergosterol

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79
Q

Polymyxins

A

Attack cytoplasmic membrane (best antifungals we have)

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80
Q

Potassium-Sparing Diuretics

A 
Act on collecting tubule and ducts
Block aldosterone (compete for Aldosterone Receptor)
- blocks Na+ channel activity and Na+/K+ channel synthesis
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81
Q

Potency

A

How small a dose you can get away with and be effective

Low potency is only a disadvantage if dose is large and awkward to administer

More potent =/= clinically superior

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82
Q

Promethazine

A

H1 Receptor Antagonist (Competitive / Reversible)

Sedative

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83
Q

Propanolol

A

β1& β2 adrenoceptor antagonist
Reduce Cardiac Output (Rate/Contractility)
Reduce Renin Release (Blood Volume/TPR)
Adverse effects:
Cold extremities (alpha1-adrenoceptor constriction)
Fatigue
Dreams / Insomnia
Bronchoconstriction (beta2-adrenoceptor blockade in airway smooth muscle)

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84
Q 
Propanolol
Timolol
Atenolol
Metoprolol
Pindolol
A

β-adrenoceptor antagonists
Reduce Cardiac Output (Rate/Contractility)
Reduce Renin Release (Blood Volume/TPR)
Propanolol/Timolol = b1 & b2
Atenolol/ metoprolol = b1
Pindolol = b1/b2 partial agonist
Adverse effects:
Cold extremities (alpha1-adrenoceptor constriction)
Fatigue
Dreams / Insomnia
Bronchoconstriction (beta2-adrenoceptor blockade in airway smooth muscle)

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85
Q

Quinidine

A

Class 1a Na+ Channel Blocker
Moderate Na block
Prolong repolarisation
Increase ERP

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86
Q

Salbutamol

A

β2 adrenoceptor agonist (Bronchial smooth muscle relaxant)
Short acting
Possible tolerance (use partial agonist to avoid tolerance)

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87
Q

Spironolactone

A

Aldosterone Receptor Antagonist
Inhibit Aldosterone action on cortical and distal tubules
K+ sparing
Reduced activation of Na+ channels
Reduced stimulation of Na+ pump synthesis

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88
Q

Statins

A

Competitive inhibitor of HMG-CoA reductase (cholesterol pathway).
Deplete Q10 (ubiquinone / coenzyme Q)
Concern that statins displose to Type II diabetes and dementia
Rosuvastatin (Crestor)
Lovastatin (Mevacor)
Pravastatin (Pravachol)
Simvastatin (Zocor)
Compactin
aviod grapefruit juice
cytochrome pathway (increase levels by antibiotics / antifungals, decrease by barbituates, phenytoin)

ADVERSE EFFECTS:
myopathy (treat with Q10)
rhabdomyolysis
renal failure, hepatitis, liver failure

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89
Q

Streptokinase

A

Activates plasminogen causing fibrinolysis
Antigenic (so single use only)
IV

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90
Q

Sympathomimetics

A

Displace Noradrenaline from vesicle and cause transport out into synampse by uptake-1 channel working in reverse
Ephidrine
Tyramine (found in foods - cheese,wine,choc)

Amphetamines (NA, 5-HT, DA release)

  • increase mood, euphoria, alertness, locomotor, behaviour, confidence
  • cause anxiety, tremor, confusion, tachycardia, BP
  • suppress appetite
  • dependence due to DA & withdrawal
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91
Q

Terfenadine

A

H1 Receptor Antagonist (Competitive / Reversible)
Non sedative
Lack anti-muscarinic activity and GIT effects

92
Q

Tetracycline

Doxycycline

A 
MECHANISM:
Inhibit protein synthesis
Bind to 16S part of 30S ribosomal subunit
Bacterial resistance via:
- inactivation of tetracycline
- Efflux
- Ribosomal protection
93
Q

Thiazide Diuretics

A 
Act on distal convoluted tubule
Inhibit Na+/Cl- cotransporter
Orally active
Max effect (4-6hours)
Duration (8-12 hours)
Adverse Effects:
gout
(as for loop diuretics)
94
Q

Tirofiban, Abciximab

A

Glycoprotein IIb/IIIa receptor antagonist
Inhibits platelet adhesion to fibrin
IV administration

95
Q

Triamterene, Amiloride

A

Diuretic
Block luminal sodium channels in collecting tubules and ducts (inhibit Na reabsorbtion and K secretion)
Trimaterene: well absorbed, 2 hour onset, 12-16 hour duration
Amiloride: poorly absorbed, slow onset, duration 24 hours

96
Q

Tubocurarine, Vecuronium

A

Pre-surgical muscle relaxant

Nicotinic AChR antagonist

97
Q

TXA2

A

Thromboxane A2
Produced by platelets
Increases platelet aggregation
vasoconstrictor

98
Q

Vancomycin

A

Blocks enzymes that catalyse construction of peptidoglycan wall - binds D-ala, D-ala
Large molecule with lots of charged groups, not soluble in lipid, acts only on gram positive bacteria, can’t penetrate cell walls

Glycopeptide antibiotic
Primarily used against resistant Gram positive bacteria (but not MRSA)

99
Q

Verapamil

A

Ca2+ Channel Blocker (significant effect on cardiac and vascular muscle)
Slow conduction velocity and increase refractoriness
Cause facial flushing, peripheral oedema, dizziness, bradycardia, headache, nausea, AV block

100
Q

Verapamil
Diltiazem
Felodipine
Nifedipine

A

Ca2+ Channel Blockers
Inhibit voltage gated L-type Ca2+ Channels (Ca2+ influx into heart)
Decrease HR, SV, CO, reduce demand, reduce supply
Primarily verapamil and diltiazem (some vascular effect)
ADVERSE: flushing, headache, oedema, bradycardia, AV block

Felodipine & Nifedipine have greater vasular effect than cardiac (can be used for hypertension)
Block Ca2+ influx into vessels
Arterial dilation, reduced afterload and demand
ADVERSE: hypotension, flushing, headache, oedema, reflex tachycardia

101
Q

Vitamin K

A

Essential for formation of clotting factors II, VII, IX, and X

102
Q

Volume of Distribution

A 
Vd = X / C
X = amount in body
C = concentration in plasma
103
Q

Warfarin

A 
Inhibit reduction of Vitamin K thereby inhibiting production of clotting factors II, VII, IX, and X
Moody Drug (strongly bound to protein)
Rapid absorbtion
Orally Active
Competition for Cytochrome P450 pathway
PT & INR used for monitoring levels

Contraindicated in pregnancy (teratogenic)

104
Q

β-adrenoceptor agonist

A

Noradrenaline / adrenaline (alpha and beta adrenoceptors)
Dobutamine (selective b1)
Amrinone (phosphodiesterase inhibitor)

105
Q

β-adrenoceptor antagonist

A

Inhibit sympathetic influence on cardiac electrical activity
Decrease Rate and conduction (SA node)
Reduce renin release (decrease blood volume & TPR)
‘olols’
Adverse effects: Bradycardia, reduced exercise capacity, hypotension, AV conduction block, bronchoconstriction, hypoglycaemia

106
Q

Glyceryl Trinitrate (GTN)

A 
Nitrate for use in angina
Smooth muscle relaxant & venodilator
1st pass metabolism
sublingual for acute attack
transdermal for prophylaxis
IV for emergency
unstable (light sensitive)

Reduces preload & cardiac work

107
Q

Isosorbide Dinitrate

A

Nitrate for use in angina
Smooth muscle relaxant & venodilator
1st pass metabolism
active metabolite - canm be given orally

108
Q

Ivabradine

A

Reduce HR
Inhibit inward Na+/K+ If current in SA
Decrease velocity of diastolic depolarization
Reduce Myocardial oxygen demand (and maxes supply)

ADVERSE EFFECTS:
brightness in visual field
conduction abnormalities

109
Q

Efficacy

A

The capacity to produce an desired effect.

(Pharmacological) The strength of the receptor activation.
(Clinical) The strength of the beneficial effect.

Emax refers to the maximum response achievable from a drug

110
Q

Angiotensin II

A

Increased sympathetic activity (vasoconstriction)
Acts on cardiovascular control centre to increase sympathetic output to heart
Na+, Cl- reabsorbtion
K+ excretion
H20 retention
Acts on adrenal cortex to increase aldosterone secretion (Na+ retention)
Acts on hypothalamus to increase ADH (vasopressin) secretion
Stimulates thirst

111
Q

Icatibant

A

Bradykinin inhibitor (B2 receptor antagonist)

112
Q

Erythropoietin

A

A glycoprotein hormone that controls erythropoiesis, or red blood cell production.
Produced by interstitial fibroblasts in the kidney in close association with peritubular capillary and tubular epithelial tubule

113
Q

Glucocorticoids

A

regulate cytokines (IL-1, TNF, IL-5)

TRANSACTIVATION
GR dimerises, 
binds GRE (promote anti inflammatory genes)
- annexin-1 (suppress phospholipase A2)
- serpin a3 (inhibit proteases)

TRANSREPRESSION
phosphorylates AP1 (activated protein 1)
bind NF-kB
Inhibits transcription of pro inflammatory genes

Used for:
Addison’s disease, asthma, topical, hypersensitivity, rheumatoid arthritis

114
Q

Omalizumab

A

Inhibit mast cell activation
Prevents IgE binding to alpha chain of FCeR1
Expensive

115
Q

Roflumilast

A

Phosphodiesterase Inhibitor
Prevents breakdown of cAMP -> amp thereby causing smooth muscle relaxation
Used in the treatment of COPD

116
Q 
What do the following target?
Tetracyclines, aminoglycosides
polyene antibiotics
penicillin, cephalosporin, vancomycin
sulphonamides, trimethoprim
quinolones, rifampicin
A

Tetracyclines, aminoglycosides - RIBOSOMES
polyene antibiotics - MEMBRANE
penicillin, cephalosporin, vancomycin - CELL WALL
sulphonamides, trimethoprim
quinolones, rifampicin

117
Q

Sulfanilamide/Sulfonamides

A 
inhibits PABA -> folate (blocks dihydropteroate synthase)
resembles PABA (p-amino benzioic acid) in folic acid
folic acid is important in bacterial pathway for creating DNA
118
Q

Trimethoprim

A

blocks dihyrofolate reductase enzyme
inhibits folate -> tetrahydrofolate (for bacterial DNA)
used for UTIs (cleared by kidney in active form)

119
Q

Cotrimoxazole

A

Sulfamethoxazole (sulfanilamide) + trimethoprim

Synergistic

120
Q

Methotrexate

A

used for cancer (high dose), rheum arth (low dose)
inhibits purine synthesis
inhibit dihyrofolate reductase (low affinity for bacterial form)
inhibits WBC & RBC and causes GIT disorders
teratogenic, therefore risk of OD

121
Q

Triple Whammy

A

Diuretic + ACE inhibitor (or AT1 antagonist) effective for hypertension
NSAID = acute renal failure because prostaglandin mediated vasodilation preserves renal blood flow.

122
Q

Anakinra

A 
IL-1 receptor antagonist
Rheumatoid Arthritis
Destructive Oesteoarthritis
Type II Diabetes
contraindicated for neutropenia
123
Q

Cimetidine, Ranitidine

A

H2 receptor antagonists
Treatetment of peptic ulcer disease
Inhibit histamine action on parietal cell
Decrease gastric acid secretion

124
Q

Omeprazole, Esomeprazole

A

Proton Pump Inhibitors (Irreversible)
Enterocyte luminal H+/K+ ATPase Inhibition
Decrease gastric acid secretion

125
Q 
Magnesium Hydroxide/carbonate/oxide/trisilicate
Sodium Bicarbonate
Aluminium Hydroxide
Calcium Carbonate
Gaviscon
A

Antacids
Neutralize gastric acid
Used in combination because of sides

Magnesium - induce diarrhoad
Sodium Bicarb - systemic alkolosis
Aluminium - constipation
Calcium - constipation & rebound acidity (gastrin release)

126
Q

Sucralfate

A

Cytoprotective

Coats stomach ulcer site and protects from acid

127
Q

Hyoscine butylbromide

A 
Muscarinic Receptor Antagonist
Reduces GI motility
Quarternary structure - not absorbed (BBB)
also known as Buscopan
Peptic ulcer treatment
128
Q

Hyoscine hydrobromide

A

Muscarinic Receptor Antagonist
inhibit SLUD (salivation, lacrimation, urination, defecation)
Tertiary amine - absorbed (BBB), sedative

effective at reducing motion sickness

Sides: dry mouth, blurred vision, urinary retention, constipation

129
Q

Mebeverine

A

Direct spasmolytic

action unknown

130
Q

Misoprostol

A

Prostaglandin E analogue
Increase mucous secretion, decrease gastric acid secretion
abortion (prostalandins increase uterus contraction/motility)
cytoprotective

131
Q

Prometazine

A

Anti-Emetic
Histamine H1-receptor antagonist
Act on chemoreceptor trigger zone outside BBB to inhibit vomiting

effective at reducing motion sickness

known as Phernergan

132
Q

Metoclopramide

Prochlorperazine

A

Anti-Emetic
Dopamine D2-receptor antagonist
Act on chemoreceptor trigger zone outside BBB to inhibit vomiting

Metaclopramide - facilitates gastric emptying (pro-motility)

  • helpful for migraine suffers (due to gastric stasis)
  • used for treatment of gastroparesis

Potent D2 antagonist (Dopamine inhibits ACh in gut)
Weaker 5HT3 antagonist
Potent 5HT5 agonist - releases ACh -> increased motility

133
Q

Dolasetron

A

Serotonin 5HT3 receptor antagonist
very few side effects, typically used in hospital
Act on vagal sensory afferents, reduce activity of messages to Chemoreceptor Trigger Zone

134
Q

Aprepitant

A

Substance p antagonist
(Neurokinin1 Receptor Antagonist)

Substance p - pain inducing substance, can cause nausea and vomiting. NK1 receptors in Chemoreceptor Trigger Zone.

135
Q

Dexamethasone

A

Glucocorticosteroid (20-30x more potent than cortisol)

Anti-inflammatory
Anti-emetic effects (Mechanism unknown)

Used for:
- Oncology, Obstetrics, High Altitude Sickness, Adrenal insufficiency and Addison’s Disease

136
Q

Docusate

A

Typically in combination with Senna

Makes faeces softer and easier to pass

137
Q

Magnesium Sulphate

A

Osmotic Laxative

causes osmotic fluid retention & colonic distension -> increased motility

138
Q

Bisacodyl

Senna

A

Stimulant laxative

Stimulates colonic myenteric nerve plexuses

139
Q

Loperamide

A 
Opioid (all opioids cause constipation including codeine)
Antidiarrhoeal
Does not cross BBB
Localised effects
Very potent at stopping diarrhoea
140
Q

Simethicone

A

Treatment of flatulence
Stays in gut (not absorbed)
Changes surface tension of air bubble causing them to coalesce into large bubbles easily passed

141
Q

Pharmacological Management of Alcohol

A

Disulfiram (antabuse) - inhibit aldehyde dehydrogenase
Naltrexone - opioid receptor antagonist - diminishes pleasure
Nalmefene - opioid receptor antagonist
Tiapride - D2 receptor antagonist - eases withdrawal symptoms
Acamprosate - GABA receptor agonist - eases withdrawal

142
Q

Orlistat

A

Reduces fat absorption
Lipase inhibitor
prevents Tryglicerides from being broken into free fatty acids

SIDES: Explosive diarrhoea, faecal fat leakage, lowered vitamin absorption

143
Q

Cyclosporin

A

Selectively takes out recently activated T Cells
Used for transplant immunosupression
Decreases IL-2 gene transcription (activation/proliferation of T Cells)

nephrotoxicity & susceptibility to viral infections

144
Q

Dopamine

A 
Catecholamine
Derived from Tyrosine, 
precursor to Noradrenaline/Adrenaline
Actions in pleasure centre of brain (nucleus accumbens & vental tegmental) - reward/dependence
Cause prolactin secretion
Frontal cortex is dopamine rich

Parkinson’s: depletion of dopamine in basal ganglia
Dopamine causes vomiting in systemic circulation
Broken down by MAO

see: Levodopa (L-DOPA)

145
Q

Benzodiazepines (Diazepam/Valium)

A

Enhance inhibitory input

  • enhanced GABA A receptor activity (act at allosteric site)
  • Increases frequency of GABA A receptor Cl- channel opening (has ceiling effect)
  • Increase POTENCY of GABA

Used For:
- Epilepsy, anxiety, sleep disorder, pre-surgery, alcohol withdrawal

Sides:
- Drowsiness, Confusion, Impaired Co-ordination, interaction with alcohol&antihistamines, withdrawal, dependence

Time:
(6-12): Oxazepam, Temazepam
(>24): Clonazepam, Diazepam

Zoplidem/Zoplicone: non-benzodiazepine’s but similar action

146
Q

Phenytoin <- most important
Ethosuximide
Felbemate

A

Reduce excitatory input

  • Phenytoin - limit excitatory nerve activation
  • good for epilepsy
  • inhibits Na+ channels
  • Na+ channel must be open to allow drug binding (i.e. enhanced during high frequency firing)
  • Ethosuximide - inhibit T-type Ca2+ channels
  • Felbemate - Inhibit NMDA receptor (on motor nerve)
147
Q

Sedative & Anxiolytic Agents

A

SEDATION
- H1 receptor antagonists are sedative

ANXIETY:

  • Serotonin
  • Noradrenaline
  • Neuropeptide Y (activation reduces anxiety)
  • β-adrenoceptor (peripheral signs only)

COMBINED:
- GABA (Benzodiazepines, Barbiturates)

148
Q

Barbiturates

A 
CNS depressant (sedation->death)
Dangerous!
  • enhanced GABA A receptor activity
  • Prolong time of GABA A receptor Cl- channel opening (overdose)
  • Increase EFFICACY of GABA

Low therapeutic Index
Addictive

149
Q

Advantages of Allosteric Modulators

A
  • Ceiling of effect of inhibitors (increased therapeutic window)
  • Positive modulation of endogenous agonist (physiological regulation continues)
  • Greater receptor subtype selectivity possible
150
Q

Aldosterone

A

released from adrenal cortex by angiotensin II, [K+], and ACTH
increase Na+ reabsorption
increase K+ secretion
spironolactone blocks activity

151
Q

Vasopressin (ADH)

A

osmoreceptors in hypothalamus detect high osmolarity
Vasopressin released from posterior pituitary
Aquaporins inserted into collecting duct epithelium
Increased water reabsorption

152
Q

Levodopa

A 
Dopamine Precursor (require dopaminergic neuron to be converted)
Peripheral conversion to dopamine: nausea, vomitting, hypotension, arrythmia
Reduces rigidity/tremors of parkinsons
Rapid absorption & short half life (1-2 hours)
Causes increased degeneration of dopaminergic neurons

Adverse Effects:
Hallucinations, abnormal movement, depression, anxiety

Interactions:
MAOI, B6, anticonvulsants, anaesthetics (inhaled)

153
Q

MDMA

A

MethyleneDioxyMetAmphetamine
Releases DA & 5-HT

Stimulant & hallucinogenic
Dependence due to DA
Increase HR, BP
Chills & sweats
Degeneration of neurons (ROS) -> mood affects
154
Q

LSD

A

Lysergic Acid Diet Hylamide

Hallucinations
Dependence & Tolerance
Cross tolerance w/o psychotomimetics
5-HT agonist

155
Q

Caffeine

A

Delays onset of sleep
Postpone boredom, inattentiveness
Anxiety, tension, tremors

Adenosine antagonist, phosphodiesterase inhibitor (HR, BP & gastric acid secretion)

No dependence but ‘weekend headache’

156
Q

Ethanol

A

CNS depressant
Inhibit Ca2+ channel opening (stop neurotransmission)
Ehnace GABA
Inhibit glutamate

Tolerance & Dependance (withdrawal)
- anxiety, insomnia, delirium, hypotension, sweating

157
Q

Cannabis / THC

A

Heightened sensory awareness and intensity
Relaxation
Dependence in heavy users

Cannabinoid receptors (GPCR)
- inhibit adenylate cyclase (similar to muscarinic receptors in heart) -> therefore inhibit inhibition

CB1 - CNS

  • impaired memory & motor control
  • catalepsy
  • analgesia
  • anti-emetic & increase appetite

CB2 - PNS receptors

  • tachycardia, sympathetic ++
  • vasodilation
  • reduced interoccular pressure (glaucoma)
  • bronchodilation
158
Q

Antidepressants

  • Tricyclic
  • MAOI
  • SSRI/SNRI
A

Tricyclic (imipramine, amitryptiline, doxepin):

  • inhibit neuronal uptake of NA & 5HT
  • poor selectivity, narrow therapeutic window & delayed clinical effects
  • muscarinic, histamine, 5-HT, α-adrenoceptor antagonist
  • sedation, hypotension, weight gain, confusion, mania, dysrhythmias

MAOI:

  • increase 5-HT, NA (and DA)
  • irreversible (phenelzine, tranylcypromine) - cheese reaction
  • reversible (moclobemide) - MAO A selective
  • hypotension, dizziness, nausea, insomnia

SSRI/SNRI (fluoxetine, paroxetine, sertraline, venlafaxine)

  • selective for 5-HT
  • few adrenergic, histaminergic, and cholinergic reaction
  • adolescent -> suicidal tendencies
  • nausea, insomnia, agitation, weight change, decreased libido
159
Q

Pegvisomant

A

GH antagonist
PEGylated (long half-life, reasonable affinity)
Used in treatment of excessive GH

Could also use somatostatin (GHIH) or dopamine agonist to inhibit GH release from anterior pituitary

160
Q

Octreotide

Lanreotide

A

Somatostatin analogues (unnatural amino acids to avoid enzymatic cleavage)
Act as Growth Hormone Inhibiting Hormones (GHIH)
Longer half lives than somatostatin

+ Dopamine antagonists (bromocriptine or cabergoline) may increase effectiveness

161
Q

PEGylation

A
  • increase size of bioactive molecule -> reduce renal clearance
  • Hydrophilicity improves solubility
  • Decreased accessibility for proteolytic enzymes
  • Occurs at lysines (important for molecules that use lysine @ binding site like GH)
162
Q

Carbimazole

A

Inhibits thyroid peroxidase
Once daily dosing

  • may lead to goiter, or hepatotoxicity
163
Q

Propylthiouracil

A

Inhibits thyroid peroxidase AND conversion of T4 to T3
2-4 doses daily

  • may lead to goiter, or hepatotoxicity
164
Q

Exogenous Liothyronine (T3)

A

Thyroid hormone
More active than T4 and acts more rapidly
Less strongly bound to proteins
1day Half Life
Levels less stable -> TSH levels less easily interpreted
Inhibits cortisol (cortisol also inhibits T3)

165
Q

Exogenous Thyroxine (T4)

A 
Thyroid Hormone
99.96% bound to plasma proteins
Vd = 10Litres
7day Half life
slow onset of action may lead to poor compliance
166
Q

Cyproterone Acetate

A

Inhibitor of androgen receptor
Blocks synthesis of mRNA for androgenic proteins

Treatment of Hirsutism, M2F, and castration

167
Q

Beclomethasone

A

Nasal spray (Beconase)

Glucocorticoid

Treatment of allergies and recurrence of nasal polyps following surgical removal

168
Q

Prednisolone

A

Glucocorticoid

Used for Asthma, Eczema, Nasal Congesion

Sides similar as for high cortisol
Progressively reduce dosage to avoid adrenal insufficiency

169
Q

Leuprorelin

A

GnRH analogue

Used to induce chemical castration via inhibition (overstimulation) of FSH and LH release
Also has application in treating breast, ovarian, and prostate cancer

170
Q

Tamoxifen

A

Selective oestrogen receptor modulator (SERM)
Breast - antagonist
Endometrium - agonist
Bone - agonist

Used in treatment of breast cancer (tamoxifen) and osteoporosis (raloxifene)
[fulvestrant is a complete oestrogen antagonist]

Adverse effects:

  • endometrial hyperplasia, polyps, cancer
  • thromboembolic events
  • thrombocytopaenia
  • occular toxicity
  • menopausal symptoms
171
Q

Letrozole

A

Aromatase inhibitor

Used in treatment of breast cancer

172
Q

Dianabol

A

Anabolic Steroid

Increases production of actin and myosin (hypertrophy)

Reduces recovery time by blocking clortisol on muscle tissue (therefore preventing catabolism)

Decrease fat by increasing BMR

Sides:
liver damage, high BP, jaundice, renal failure, acne
Delusions, jealousy, paranoia, irritability
Reduced sperm count, shrinking testes, infertility, prostate cancer, baldness
Facial hair growth, deepened voice, oligomenorrhoea
Stunted growth, developmental problems

173
Q

Ciclesonide

A

Third generation glucocorticoid

Reduced systemic effects after inhalation

  • activation in lungs (not mouth/larynx)
  • lipophillic (retained in tissues)
  • low bioavailability (hepatic 1st pass metabolism)
  • highly protein bound
174
Q

Allopurinol

A

Xanthine Oxidase inhibitor
Prevents the formation of Uric Acid
Used in the treatment of Gout

175
Q

Insulin

  • long acting
  • short acting
A

Isophane
Glargine
Detemir

Neutral
Glulisine
Lispro
Aspart

176
Q

Sulphonylureas & Meglitinides

A

Used for Type II Diabetes (relative lack of insulin)

Inhibit pancreatic β-cell K+ channel

  • > depolarisation and Ca2+ entry
  • > insulin secretion

HL: 6-24 hours
Can cross placenta (contraindicated in pregnancy)
Excreted via kidney

SIDES: hypoglycaemia, weight gain

177
Q

Biguanides (Metformin) & Thiazolidinediones

A

Used for Type II Diabetes (Insulin resistance)

Increase insulin-mediated peripheral glucose uptake
Reduce hepatic glucose production
Decrease carbohydrate absorption, LDL & TAG levels
Activates AMP Kinase (increases metabolism)

SIDES: GI disturbance, lactic acidosis, weight loss, contraindication w/ renal dysfunction

178
Q

Alpha-glucosidase inhibitors

A

Block enzymes of digestion and absorption in small intestine
Not absorbed from GI

SIDES: flatulence, loose stool, abdo pain / discomfort, contraindicated w/ IBD or cirrhosis

179
Q

Exenatide

A 
Incretin for treatment of Type II Diabetes
GLP-1 agonist
increase glucose-mediated insulin
decrease glucagon
slow GI emptying
decrease appetite

SIDES: nausea, diarrhoea, vomiting, weight loss, immune reaction (antibody complex), pancreatitis, neoplasia (endocrine)

180
Q

DPP-IV Inhibitor

A

Treatment of Type II Diabetes

Increase native GLP-1 levels
Increase insulin
Decrease glucagon
only as adjunct to diet and exercise!

SIDES: URTIs, headaches, hypersensitivity, pancreatitis, contraindicated w/ insulin -> hypoglycaemia

181
Q

Phentermine (Duromine)

A

Used for Obesity

Amphetamine Derivative
Increases NA, DA, & 5HT (competes/blocks reuptake)
Suppresses appetite

Only useful in short term (tolerance & addiction)

SIDES: Increased BP, HR, insomnia, nervousness, headache, dry mouth

182
Q

Topiramate (Topamax)

A 
Used for Epilepsy / Migrane / Obesity
mechanism unknown (suppress appetite, increase energy expenditure)

SIDES: dizziness, taste alteration, teratogenic

183
Q

5-flurocystosine

A

Prodrug activated by fungi and converted to 5-Flurouracil

5-FU also used in cancer treament

184
Q

Drug classes used in bone disorders (antiresorptive vs anabolic)

A

ANTIRESORPITIVE

  • Bisphosphonates
  • SERMs
  • RANKL inhibitors

BONE ANABOLIC AGENTS

  • PTH
  • Oral Calcium
  • Oral Vitamin D analogues
  • Calcitonin
185
Q

Bisphosphonates (e.g. Alendronate)

A

Enzyme resistant analogue of pyrophosphate
Incorporated into bone matrix and ingested by osteoclasts during resorption
Inhibit recruitment of osteoclasts
Promote apoptosis of osteoclasts
= reduced fracture risk

Weekly administration. Poor Absorption. Risk for oesophagitis (due to reflux) and oesophageal cancer

186
Q

Raloxifene

A

Selective oestrogen receptor modulator
Breast & endometrium - antagonist
Bone - agonist

Used in treatment of osteoporosis instead of HRT

Oestrogen decreases osteoclast proliferation, differentiation and activation, and promotes apoptosis
Increases lifespan of osteoblasts and osteocytes
Maintains bone mass and slows bone loss
Increased risk of CVD

187
Q

Denosumab

A

RANKL inhibitor
Reduces osteoclastic activity
Treatment of osteoporosis

188
Q

Rimonabant

A

CB1 antagonist
Anorectic
Withdrawn - suicidal thinking

189
Q

Effect of Exercise on Exogenous Insulin

A

Plasma [insulin] increased

dependent on:
type, duration, intensity
muscle mass
level of fitness
carbohydrate supplementation
can cause hyperglycaemia or hypoglycaemia
190
Q

Effect of Exercise on GTN (transdermal)

A

Plasma [GTN] increased

mechanisms:
increased skin blood flow = increased transdermal absorption
excess vasodilation may cause hypotension

191
Q

Effect of Exercise on Salbutamol

A

Plasma [salbutamol] increased

mechanisms:
increased resp rate
increased pulmonary blood flow
increased epithelial permeability

192
Q

Effect of Exercise on Oral Drugs (GI)

A

inhibition of gastric emptying (reduced drug delivery)
increased intestinal motility (less time for absorption)
decreased splanchnic blood flow

193
Q

Effect of Exercise on Digoxin

A

Plasma [digoxin] lowered
Muscle [digoxin] increased

mechanism:
increased binding to skeletal muscles
therefore reduced ability to control heart rate

194
Q

Effect of Exercise on Warfarin

A

Plasma [warfarin] decreased

mechanism:
increased sweating
lowered blood volume
increased binding to albumin
= decreased FREE warfarin
195
Q

Effect of Exercise on β-blockers

A 
Plasma [propanolol] increased 
    - reduced hepatic clearance)
Plasma [atenolol] increased 
    - reduced renal clearance
Plasma [carvedilol] same
196
Q

Azithromycin

A

Treatment of Chlamydia (reticulate form) and Gonorrhoea
Attains high intracellular concentrations

Macrolide - Binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA

197
Q

Acyclovir

A

Nucleoside analog without 3’ -OH
used in treatment of herpes
herpesvirus thymidine kinase phosphorylates nucleoside to nucleotide
DNA polymerase adds nucleotide into viral DNA and ends transcription
valacyclovir similar but has Valine group which is removed by cellular enzymes (better bioavailability)

198
Q

Ribavirin

A 
Nucleoside analog with 2' -OH
works on DNA and RNA viruses
 RSV
 Influenza
 Haemorrhagic fevers (ebola)
 Hepatits C
199
Q

HIV - Fusion/Entry Inhibitors

A
  • bind CD4 and inhibit
  • bind CCR5 (Maraviroc) or CXCR4 and inhibit
  • bind gp41 trimer on HIV (Enfuviritde & T20 fusion inhibitor)
200
Q

HIV - Reverse Transcriptase Inhibitors

A

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

  • nucleoside analogues (phosphorylated by viral enzyme)
  • reduce infection of new cells but can’t eliminate virus
  • Azidothymidine (thymidine analogue lacking 3’ -OH )

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
- directly inhibit reverse transcriptase enzyme by other mechanisms

201
Q

HIV - Integrase inhibitors

A

Inhibits integration of cDNA into cellular DNA

Raltegravir binds to active site of integrase enzyme
cDNA degrades or forms dead-end circle

202
Q

HIV - Protease inhibitors

A

Saquinavir and Indinavir
bind to active site of protease enzyme
prevent cleavage of polyproteins into matrix, capsid, enzymes etc.
virus doesn’t mature so particles are non-infectious

203
Q

Emexestane

A

Aromatase inhibitor
(aromatase high in breast and adipose tissue)
- reduced synthesis of oestrogens

BENEFITS:

  • reduced incidence of contralateral breast cancer
  • reduced thromboembolic events
  • reduced endometrial cancer incidence

RISKS:

  • increased bone loss & fracture risk
  • increased arthralgia
  • poorer lipid profile, hepatic steatosis, metabolic syndrome
  • menopausal signs
204
Q

Finasteride

A

5a-reductase inhibitor

USES:

  • benign prostatic hypertrophy
  • hair loss

SIDES:

  • impotence, decreased libido
  • breast enlargement, tenderness, cancer
205
Q

Cyproterone

A

steroidal androgen antagonist
deriverative of progesterone
antiandrogenic

USES:

  • prostate cancer
  • androgenisation in female
  • oral contraceptive
  • M2F

ADVERSE EFFECTS:

  • higher risk of venous thromboembolic event
  • cognitive changes, fatigue, odeema
  • reduces spermatogenesis
206
Q

Flutamide

A

non-steroidal androgen antagonist

USES:
- metastatic prostate cancer (+GnRH agonist)

ADVERSE EFFECTS:

  • diarrhoea, anaemia
  • oedema, dizziness, blurred vision
207
Q

ethinyloestradiol

A

synthetic oestrogen used in oral contraceptives

208
Q

norethisterone, levonorgestrel

A

Synthetic progesterones used in oral contraceptive pills

Slightly androgenic (acne, hirsutism)

Morning after pill is high dose (10x) of levonorgestrel

209
Q

drospirenone

A

Synthetic progesterones used in oral contraceptive pills

Antiandrogenic

Mild diruetic (spironolactone derivative)

210
Q

Codeine

A 
Inactive
Demethylated in liver (to form morphine)
Morphine acts on u-opioid receptors
Greater bioavailability than  morphine
Suppresses cough
Drowsiness/Sedation/Ventilatory depression
Decreases gut motility (causing constipation)
Can cause nausea/vomiting

combined with naloxone = Targin

211
Q

Prialt

A

Analgesic (neuropathic pain)

Blocks subunit of pre-synaptic calcium channel

Given intrathecally (otherwise has effects on sympathetic nerves)

212
Q

Lyrica, Neurotonin

A

Analgesic (neuropathic pain)

Reduces cell surface expression of pre-synaptic calcium channel

Effective for only 50% of patients

213
Q

Oral Contraceptive Mechanism

  • oestrogen
  • progesterone
  • adverse effects
  • benefits
A

OESTROGENS

  • negative feedback on anterior pituitary
  • inhibit FSH therefore inhibit ovulation

PROGESTOGENS

  • negative feedback on anterior pituitary and hypothalamus
  • inhibit LH
  • modifies cervical mucous (inhospitible for sperm)
  • changes properties of endometrium (unfavourable for implantation)
  • interfere with contractions of fallopian tubes

ADVERSE EFFECTS:

  • hypertension
  • venous thromboembolism (risk proportionate to dose)
  • cancer (oestrogen only)
  • nausea/vomiting
  • flushing
  • headache
  • decreased libido
  • depression/irritability/fatigue

BENEFITS:

  • decreased cancer risk w/ progestogen (endometrial, ovarian, colorectal, breast)
  • decreased risk of bone fracture
  • protective for anaemia (reduction in oligomenorrhea)
214
Q

Herceptin

A

binds HER2

Inhibits epidermal growth factor binding leading to cell death

Expensive

Used for breast cancer treatment

215
Q

Oxytocin

A
  • used in obstetric haemorrhage
  • IV or IM administration
  • stimulates smooth muscle contraction
    SIDES: hypotension, tachycardia, water intoxication
216
Q

Ergometrine

A
  • used in obstetric haemorrhage (avoided with pre-eclampsia)
  • IV or IM administration
  • stimulates smooth muscle contraction (uterus and vascular smooth msucle)
    SIDES: hypertension, nausea, vomiting
217
Q

Labetalol

A
  • alpha-antagonist (vasodilation)
  • non selective beta-antagonist (prevent increased HR)
  • used for pre-eclampsia
218
Q

HIV treatments

  • Miraviroc
  • Enfuvirtide
  • Zidovudine/AZT
  • Nevirapine
  • Raltegravir
  • Saquinavir
A

Prevent binding to CCR5 (maraviroc)

Prevent hiv fusion to gp41 (enfuvirtide)

Nucleoside Reverse Transcriptase Inbitors (zidovudine/AZT)

Non-Nucleoside Reverse Transcriptase Inbitors (nevirapine)

Prevent Integrase (raltegravir)

Prevent viral polyprotein clevage and maturation (saquinavir)

Highly Active Anti-Retroviral Therapy = combination of above

  • avoid resistance
  • combination of partial antagonists
  • inhibit cytochrome metabolism of active compounds
219
Q

Targin

A 
Combination analgesic
Oxycodone 
 - opioid analgesic
 - u-receptor agonist
Naloxone
 - used to treat opioid intoxication
 - u-receptor antagonist
 - primary action in GI tract
 - prevent constipation of oxycodone
220
Q

Transplant Immunosuppressive Drugs

A

Inhibit cytokines (prednisolone)
Cytotoxic (azathioprine)
Calcineurin inhibitors (cyclosporin)
Cytokine receptor antagonist (daclizumab anti-IL2)
T-lymphocyte depletion (anti-thymocyte globulin)
Inhibition of co-stimulation (abatacept anti-CTLA4)

221
Q

Toxin types in Australian animal venoms

A

Neurotoxins

  • ticks (ascending paralysis over days)
  • snakes (neuromuscular block)
  • death adder (no coagulopathy)
  • redback (enhanced neurotransmitter release, sweating at bite site, painful)
  • funnel web (fulminant, stimulate CNS, tachycardia, raised ICP, CNS depletion and hypotension)

Cytotoxins (necrosis)
- box jellyfish (cardiotoxicity)

Myotoxins
- brown snake (tiny fangs, may have no pain)

Anti/pro-coagulants

  • butterfly/caterpillars/moth
  • snakes (clotting & depletion of clotting factors = bruising and oozing at puncture site)
  • venom allergy
  • ants
  • bees
222
Q

Envenomation Investigations

A

Snake venom detection kit (bite site > urine > blood)
Check clotting & fibrinogen
d-dimer (fragmentation of clot)
Renal function (rhabdomyolysis - K+ & CK)
Haemolysis

223
Q

Cephalosporins

A

MECHANISM:
Beta lactam - disrupt synthesis of peptidoglycan for cell wall

BACTERIA:
GPs (1st gen)
GPs & some GNs (2nd gen)
GNs & some GPs inc. gonorrhea and syphilis (3rd gen)
Pseudomonas (4th Gen)
MRSA (5th gen)
NAMES:
Cefazolin
Cefalexin
Cefotoxin
Cefixime
Cefotaxime
Ceftriaxone (STIs)

SIDES:
GI upset, nausea, diarrhea, allergy

224
Q

Macrolides

A

MECHANISM:
Bind to 50s ribosome

BACTERIA:
Strep
Syphilis/Chlamydia
URTIs/LRTIs

NAMES:
Azithromycin

SIDES:
Nausea, Hearing Loss, Jaundice

225
Q

Penicillins

A

MECHANISM:
Beta-lactam - disrupt synthesis of peptidoglycan cell wall

BACTERIA:
Strep
Syphilis

NAMES:
Amoxicillin
Ampicillin
Carbenicillin
Flucloxacillin
Methicillin
Penicillin G
Penicillin V
Piperacillin
Ticarcillin

SIDES:
GI upset, allergy

226
Q

Quinolones

A

MECHANISM:
Inbibit DNA gyrase - thereby inhibiting DNA replication

BACTERIA:
UTIs
pneumonia
Gonorrhoea

NAMES:
Ciprofloxacin

227
Q

Amantadine / Rimantadine

A

Antivirals for treatment of influenza

Block M2 ion channel thereby inhibiting uncoating of virus/endosome

MD1 (11 decks)

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