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Flashcards in General Drugs Deck (102):
0

Pilocarpine

Non selective musc agonist
Alkaloid
Glaucoma
3-4 hours

1

Bethanechol

M3 selective agonist
Choline ester
Bladder emptying and gi motility
3-4 hours

2

Physostigmine

Reversible anticholinesterase
Donate carbamyl group to active site
Glaucoma and atropine poisoning

3

Ecothiopate

Organophosphate
Irreversible anticholinesterase
Leave large blocking group resistant to hydrolysis
Glaucoma

4

Hexamethonium

Nic antagonist
Blocks ion channel
1st antihypertensive

5

Trimetaphan

Nic antagonist
Works at receptor
Hypotension during surgery

6

Pralidoxime

Acetylcholinesterase poisoning

7

Botulinum

Interferes with snare complex, stopping Ach being released
Most toxic protein

8

Atropine

Musc antagonist
Anaesthetic premed
IBS

9

Tropicamide

Musc antagonist
Examination of retina

10

Ipratropium bromide

Asthma copd
Musc antagonist
Highly charged localised in lungs

11

Hyoscine

Musc antagonist
Motion sickness and Parkinson's

12

Statins

Inhibit HMG-Coa reductase
Hepatocytes up regulate LDL receptors so more removal of LDL from blood
Increase hdl too

13

Bile Acid Sequestrants

Bind to bile acids and prevent reabsorption. Liver increases synthesis and excretion of cholesterol from liver. Not work too well on triglycerides.

14

Nicotinic acid

B complex vitamin
Lots of effects on hdl LDL and tg's
Expensive adverse effects difficult dosing

15

Fibrates

Triglyceride lowering drugs
Only moderately reduce LDL
Act on ppar receptors
Not usually used cos effects on inflamm thrombosis etc

16

Ezetimibe

Activated as glucoronide, secreted in bile into gi tract whereby blocks cholesterol absorption
Reduce LDL significantly

17

Torcetrapib

Cetp inhibitor
But increase mortality cos increases bp increased aldosterone

18

Ibuprofen and indomethacin

NSAIDS
Inhibit cox 1 and 2 reversibly

19

Celecoxib

NSAID
Selective cox 2 inhibitor
Fewer ulcers but more cvs problems

20

Aspirin

NSAID
Selective cox 1 inhibitor
Binds irreversibly
Reduces platelet aggregation

21

Paracetamol

Analgesic and antipyretic
Treat overdose with NAC or methionine

22

L dopa with carbidopa

Can cross bbb
With peripheral DOPA decarboxylase inhibitor
Sinamet
Nausea, schizo, dyskinesias, on off effects

23

Doperidone

Dopamine antagonist peripheral acting to stop nausea

24

Bromocriptine Cabergoline Pergolide Ropinerol

Dopamine agonist
D2 receptors
Longer diration of action than l dopa
Less dyskinesias

25

Deprenyl (selegiline)
Resagiline

MAO B inhibitor

26

Tolocapone and entacapone

COMT inhibitor
Stop 3 OMD production which would otherwise compete with l dopa to get into brain

27

Lidocaine

Amide local anaesthetic
2 hours half life
Hepatic n dealkykation
Cns up cvs down

28

Cocaine

Ester local anaesthetic
Plasma and liver esterases
1 hour half life
Cns up cvs up
Blocks uptake 1
Indirectly acting sympathy mimetic

29

Muscimol

GABA a agonist

30

Bicuculline

Comp antagonist for GABA a

31

Baclofen

GABA b agonist
Muscle relaxant
Spasmolytic drug

32

Saclofen

Competetive antagonist for GABA b

33

Dabigatran

Factor 2a inhibitor

34

Rivaroxaban

Factor 10a inhibitor

35

Heparin

Activates anti thrombin 3

36

Dalteparin

Low molecular weight heparin
Activate antithrombin 3 and inhibit factor 10a

37

Warfarin

Vitamin k antagonist

38

Clopidogrel

Adp receptor antagonist

39

Abciximab

Gp 2b 3a antagonist

40

Alteplase

Thrombolytic
Tissue type plasminogen activator

41

Flumazenil

GABA a receptor antagonist
Counteract benzos

42

Thiopentone

Barb
Anaesthetic

43

Amobarbital

Barb
Severe intractable insomnia
20-25 hour half life

44

Diazepam

Long acting benzo
32 hour half life
Anxiolytics
Spasmolytic

45

Temazepam and oxazepam

Benzo short acting
8 hour half life
Sedative and hypnotic

46

Nitrazepam

Benzo
Daytime anxiolytics effect
28 hours

47

Zopiclone

Short acting 5 hours
Acts at benzo receptors
Minimal hangover but still dependency
Sedative hypnotic

48

Propranolol

Beta blocker non selective
Anxiolytics to improve physical symptoms of tachycardia and tremor
Can cross placenta and cause teratogenesis
Affects heart rate co when exercising
antiarrythmic

49

Buspirone

Serotonin agonist
Anxiolytics
Few side effect
Slow onset of action

50

Naloxone

Opioid antagonist
Iv

51

Morphine

Opiate
40-50 percent bio available
30mins for onset
First pass metabolism
Tertiary nitrogen and 3 and 6 hydroxyl groups

52

Codeine

Opiate
Methylmorphine at 3 position
Prodrug
5-10percent converted to morphine by activating and deactivating metabolism

53

Heroin

Opiate
Diacetylmorphine
More lipid soluble get Into brain faster
50-100percent bio available
Plasma esterases

54

Fentanyl

Opiate
50-100percent bio available
Quickly oxidised metabolised In gut

55

Methadone

Opioid
Most lipid soluble one
Dissolves in fat long half life

56

Phenylephrine

A1 agonist
Vasoconstrictor stop superfici bleeding
Mydriatic eye drops
More resistant to COMT
Nasal decongestant

57

Clonidine

A2 agonist
Hypertension and migraine
Reduces sympathetic tone

58

Isoprenaline

Non selective beta agonist
Less susceptible to uptake 1 and Mao
Cardiogenic shock
Can get reflex tachycardia and smdyarhythmias

59

Dobutamine

Beta 1 agonist
Cardiogenic shock and lacks reflex tachy
Half life only 2 mins

60

Salbutamol

Beta 2 agonist
Ventolin
Resistance to Mao and COMT
Treat asthma and threatened uncomplicated premature labour
Can get reflex tachy

61

Tyramine

Dietary amino acid in cheese red wine soy sauce
FalseNT indirectly acting sympathy mimetic
Competes with NA to be packed into vesicles so more NA released
If take MaO inhibitor get hyperT crisis

62

Adrenaline

Allergic and anaphylaxis
Pulmonary obstructive condition Cardiogenic shock
Spinal anaesthesia to maintain bp
Prolong la
Glaucoma

63

Dantrolene

Spasmolytic

64

Tubocurarine and atracurium

Non depolarising nmb
Comp nic antagonists -alkaloid
Flaccid paralysis - eye muscles, small muscles of face limbs pharynx, resp muscles
Surgery, artificial ventilation - 40-60min
Care if hepatic renal impaired
Reverse by anticholinesterase

65

Suxamethonium

Depolarising nmb - agonist
Extended ep depolarisation - dep block phase 1
Fasciculatiins then flaccid paralysis
Short 5 min paralysis
Metabolised by pseudocholinesterase
Et intubation and muscle relaxant for ect

66

Mannitol

Osmotic diuretic
Whole tubule

67

Acetazolamide

Carbonic anhydrase inhibitor
Acts on pct

68

Frusemide

Loop diuretic
Ascending loop

69

Bendrofluazide

Thiazides
Acts on early dct

70

Amiloride

Potassium sparing diuretic
Late dct and collecting duct

71

Spironolactone

Potassium sparing diuretic
Late dct and collecting duct

72

Promethazine

Anti emetic
Comp antagonist at h1 receptors
Motion sickness, disorders of labyrinth, heperemis gravidarum
Allergy anaphylaxis

73

Metoclopramide

Anti emetic
Dopamine 2 receptor antagonist
Acts at ctz and increase gi motility and emptying
Cancer chemo, uraemia and go disorders
More prolactin
Useful for acid reflux disease

74

Ondasetron

Serotonin antagonist
Cancer chemo vomiting
Headache flushing constipation

75

Atenolol

B1 selective blocker
Heart and kidneys
Still not safe for asthmatics

76

Labetolol

A1 and b1 antagonist
Don't really use now
Lowers bp, effect on heart wanes with chronic use

77

Phentolamine

Non selective alpha antagonist
Vasodilation, bp falls
Reflex tachy
Increase gi motility
Don't really use

78

Prazosin

A1 antagonist
Vasodilation fall in bp
Less reflex tachy
Co decreases
Get postural hypotension
Decrease LDL and increase hdl

79

Methyldopa

False NT antagonist
Antihypertensive
Not broken down by mao so accumulates and displaces NA from vesicles
Less active at a1 more active on a2
Use for renal/cerebrovascular insufficiency or pregnant

80

Omeprazole

Ppi
Inhibits acid production by over 90 percent
Irreversible inhibitors of h k atpase
Inactive at neutral ph
Weak base

81

Cimetidine and ranitidine

Histamine type 2 antagonist
Inhibit gastric acid production by 60 percent

82

Metronidazole

Antibiotic against anaerobic bacterial and protozoa
Interferes with alcohol metabolism

83

Amoxycillin

Broad spectrum antibiotic

84

Clarithomycin

Antibiotic with macrolide structure
Inhibits translocation of bacterial tRNA

85

Sucralfate and bismuth chelate

Polymer with aluminium hydroxide and sucrose octa sulphate
Acquires neg charge in acid, binds to pos charge groups - gel like complex
Increase pg, mucous and bicarbonate and reduce h pylori

86

Misoprostol

Prostaglandin analogue
Maintain mucosal barrier
Use when taking NSAIDs
Don't use In pregnancy cause cause uterine contractions

87

Antacids

Sodium bicarbonate rapid
Aluminium hydroxide and mag trisilicate slow
Neutralise acid reduce pepsin activity
Dyspepsia

88

Mesalazine and olsalazine

Aminosalicylates
Anti inflamm
Induce and maintain remission in uc
May help surgically induced remission in crohns
O - prodrug needs to activated by colonic flora, M- works in small or large int

89

Prednisolone, fluticasone and budesonide

Glucocorticoids steroids
Anti inflamm and immunosuppressive
Good for crohns, ok for uc
Unwanted effects though

90

Azathioprine

Immunosuppressive
Maintain remission in crohns also for uc
Better than budesonide
Prodrug activated by gut flora to 6 mercaptopurine which interferes with purine biosynthesis
Metabolised by xanthine oxidase (inhibitor is allopurinol)

91

Methotrexate

Folate antagonist
Reduces thymine and other purine synthesis
Significant unwanted effects
Ibd

92

Infliximab

Anti tnf alpha
Ibd and ra
Very long half life

93

Verapamil

Phenylalkylamine
Rate slowing ca antagonist
Cardiac and smooth muscle actions
But mainly cardiac
Anti arrhythmic

94

Diltiazem

Benzothiazepines
Ca antagonist
Rate slowing cardiac and smooth muscle

95

Amlodipine

Ca antagonist
Non rate slowing
Smooth muscle more potent
No effect on heart
Dihydropines

96

Adenosine

Anti arythmic
sVT
Short lived so safer than verapamil

97

Amiodarone

Anti arythmic
Multi ion channel block
Accumulates in body long half life photosensitive skin rash

98

Digoxin

Cardiac glycoside
Inhibit NA k pump positive inotrope
Central vagal stimulation for increased refractory period less conduction through av mode decrease heart rate
Atrial fib

99

Enalapril

Ace inhibitor somatic form
For hyperT heart failure mi diabetic nephrophathy
Give cough hypoT

100

Losartan

Angiotensin receptor blocker block type 1 receptors
Better tolerated than ace inhibitors

101

Sumitriptan

Serotonin agonist
Constricts large arteries and inhibit trigeminal
Treat migraine
Dizziness drowsiness