Pharmacology Flashcards

(85 cards)

1
Q

Gq

Contraction of vascular smooth muscle

A

a1

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2
Q

Gi

Inhibition of noradrenaline release

A

a2

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3
Q

Gs

Positive inotropic and chronotropic effect

A

B1

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4
Q

Gs

Relaxation of bronchial smooth muscle

A

B2

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5
Q

Gq

Increased gastric acid secretion

A

M1

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6
Q

Gi

Decreased HR

A

M2

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7
Q

Gq
Increased saliva
Visceral smooth muscle contraction

A

M3

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8
Q

Gs stimulates

A

Adenylyl cyclase

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9
Q

Gq

A

Stimulation of phospholipase C

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10
Q

Gi

A

Inhibition of adenylyl cyclase

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11
Q

Drug elimination rate independent of dose

A

Zero order kinetics

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12
Q

Drug elimination proportional to dose

A

First order kinetics

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13
Q

What is the steady state

A

Rate admin = rate elimination

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14
Q

Phase I metabolism

A

Oxidation, hydrolysis and reduction

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15
Q

Phase II metabolism

A

conjugation to make more hydrophilic

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16
Q

Examples of biguanides

A

Metformin

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17
Q

Action of biguanide

A

Decreases hepatic gluconeogenesis via AMP protein kinases
Increases peripheral uptake
Reduces carb absorption
Increases fatty acid oxidation

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18
Q

Indications for metformin

A

1st line T2DM
Protective against risks
WEIGHT LOSS
No hypoglycemia risk

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19
Q

Side effects of metformin

A

GI upset

Lactic acidosis

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20
Q

Sulfonylureas examples

A

Tolbutamide

Gliclazide

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21
Q

Sulfonurea action

A

Displaces Mg-ADP on SUR1 from Katp channel
B cell depolarises
Stimulates insulin release

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22
Q

Sulfonylurea indications

A

Add on T2DM

MODY ( HNF-1a)

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23
Q

Sulfonylurea side effects

A

Weight gain
HYPOglycemia
LFT derangement

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24
Q

Thiazolidione example

A

Pioglitazone

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25
Thiazolinediones action
PPARy activator to: Increase insulin signalling (more glucose uptake) Increased uptake and metabolism of FAs (reduce resistance)
26
Thiazolinedione usage
Add on in T2DM (HbA1c reduced by 0.6-1.5%)
27
Contraindications of thiazolinediones
3-5kg weight gain Fracture risk Hepatotoxic fluid retention
28
SGLT-2 inhibitors
Dapagliflozin Canagliflozin Empagliflozin
29
SGLT-2 inhibitor mechanism
blocks SGLT-2 to prevent glucose reabsoprtion in PCT
30
Uses
Add on T2DM
31
sglt-2 side effects
UTIs | Ketoacidosis
32
DPP4 inhibitors
'gliptins'
33
DPP4 inhibitor action
inhibits DPP4 enzyme so GLP-1 and GLP can work longer | Increases insulin and decreases glucagon
34
DPP4 uses
alone/ add on to T2DM
35
DPP4 side effets
Nausea
36
GLP-1 receptor agonists
extenatide | Liraglutide
37
GLP-1 action
Mimics GLP-1 to incrase insulin secretion | resistant to DPP4
38
Uses of GLP-1
Good for meal relateed hyperglycemia
39
a Glucosidase inhibitors
acarbose voglibose migitiol
40
a Glucosidase action
inhibits a glucosidase to decrease starch breakdown | Reduced glucose absorbed
41
Acetazolimide class
CA inhibitor
42
CA inhibitor action
inhibits CA to increase HCO3 so more Na+ excreted
43
CA inhibitor usage
glaucoma (reduced intraocular pressure)
44
Furosemide | Bumetinide
Loop diurectics
45
Loop diuretics action
Inhibits triple transport so less Na, K and Cl pumped out Less water leaves descending limb More K, Mg, Ca loss
46
Loop diuretics usage
Salt and water overload | Hypertension
47
Lopp diuretics side efects
``` Dont use when BP low Low Na, K, metabolic acidosis Gout Hearing loss ```
48
Thiazide diuretics
``` Bendroflumethiazide also: Chlortalidone Indapamide Metolozone ```
49
Action of thiazides
Na-Cl in DCT More Na (and K) pissed out more water pissed out Mg loss
50
Thiazide action
mild heart failure Hypertension renal stones Diabetes insipidus
51
Side effects of thiazides
``` Decreased Na, K, Mg Gout Metabolic acidosis ED Hypotension ```
52
Potassium sparing diuretics
Amiloride and triamterene | Spironolactone and eplerenone
53
Use of K sparing ABs
Heart failure Hyperalosteronism Hypertension
54
Action of K sparing ABs
Amiloride and triametrene: Block apical Na channels to reduce uptake (but no K loss as its the collecting ducts) Spironolactone Aldosterone antagonists to prevent salt and water uptake (No Na reabsorption so no K loss)
55
When to avoid K sparing drugs
Hypokalaemia Severe renal impairment Addisons
56
What is mannitol
Osmotic diuretic Increases osmolarity in PCT to reduce movement of water Maintains renal flow and reduces ICP
57
Vaptans
Conivaptan | Tolvaptain
58
Vaptan action
Antagonists of V receptors on aquaporin 2 channels to prevent ADH action Water excreted without Na loss
59
When are vaptans used?
SIADH Hypervolaemia Hyponatraemia
60
Uricosuric agents
probenicid Block reabsorption of urate in PCT used for gout
61
Antimuscarnics
oxybutynin tolteridione Solfenacin Prevent overactive bladder contracting
62
Side effects of antimuscarinics
Heat stroke Dry mouth Urinary retention
63
B3 andrenergics
Mirabegnon Relaxes detrusor used in urge incontinence
64
A blocker
Tamulosin A1 receptor antagonist to prostate to relax muscles Used in kidney stones and urinary retention
65
A blocker side efects
Allergy | Hypotension
66
Duloxetine
Stress incontinence
67
NSAID examples
Aspirin ibuprofen naproxen diclofenac
68
NSAID mechanism
Block COX to prevent PG release so reduced pain sensation and inflammation
69
Side effects of NSAIDs
GI problems Renal impairment Wheeze Rash
70
DMARD examples
``` MTX SFZ Azathioprine lefluonimide HCQ ```
71
DMARD use
Reduce rate of joint damage
72
Side effects DMARDS
Liver damage (monitor LFTs) ulcers TERATOGENIC
73
Biologics examples
-imabs
74
Biologics action
Inhibit immune system (generally TNF) | used in autoimmune arthritis coniiditons
75
Side effect of biologics
TB reactivation
76
Urate lowering drugs
Allopurinol | Febuxostat
77
Action of urate lowerig drugs
xanthine oxidase inhibitors so no urate synthesis
78
Use of urate lowering drugs
Chronic gout
79
Side effects of urate lowering drugs
Azathioprine interactons
80
Acamprosate mechanism and use?
``` Stabilises chemical signalling alcohol dependence (reduces pleasure) ```
81
Naltrexone mechanism and use
Opioid receptor antagonist Reduces amount and frequency of drinking DOnt give in liver failure
82
Dilsulfiram mechanism and use
Inhibits acetaldehyde dehydrogenase enzyme so hangover symptoms (nausea, vomiting tc) when drinnking 2nd line alcohol dependence
83
Pabrinex and thiamine mechanism and use
Thiamine supplements | Wernicke-korsakoff syndrome (give with glucose infusion)
84
Diazepam mechanism and use
GABA A receptor modulator Makes neurone less likely to fire Calming effects
85
Side effects of diazepam
confusion sedation amnesia falls