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PHAL211 > Drugs > Flashcards

Drugs Flashcards

1
Q

Drug misuse

A

any drug taking that causes physiological or mental harm

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2
Q

Tolerance

A

reduction in effect of a drug with repeated administraion (metabolism, receptors-number affinity, efficacy), adaptive or maladaptive

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3
Q

Drug dependence

A

withdrawal symptoms alleviated by further drug use

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4
Q

NSAID

A

non steroidal anti-inflammatory drug

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5
Q

Nociceptors

A

sensitisation nerves

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6
Q

COX

A

cyclo oxygenase - archidonic acid ->PL/PG, COX1 (PGE1 , PGE2, PGI2) protect against ulcers, COX2 inducible isoform-less GI side effects

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7
Q

PG

A

phospholipids -> prostaglandins

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8
Q

Opioids

A

Opioids - drugs that act on opioid receptors in CNS, endogenous opioids=endorphines, analgesia, sedation, respiratory depression, nausea, constipation,

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9
Q

Opioid receptors

A

nociceptor signals at sensory neuron termini (Gi), u and S and k.

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10
Q

Cannabinoids

A

CB1 gi receptors, THC

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11
Q

Migraines

A

severe headache, hypersensitivity, nausea, aura, episodic or chronic. Trigeminivascular (trigeminal sensory nerve, innervate meningal blood vessels)

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12
Q

Triptans

A

oral, subcutaneous, intranasally. Slective agonist for 5HT1B/1D (Gi) receptors in cranial blood vessels -> vasoconstriction -> decrease neurotransmitter release

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13
Q

Ditans

A

5HT1F - CNS + trigeminovascular system. Avoids 1B side effects. Gi-inhibition of presynaptic release and post signalling

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14
Q

CGRP

A

neuropeptide in trigeminal neurons. Reduce release for pain transmission= CGRP antagonist or antibodies that bind to peptide (migraines)

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15
Q

Diabetes mellitus

A

insulin deficiency (type 1), insulin resistance (type 2) -> stroke, loss of feet, skin, high bp. Gluocse monitors, check ups, medications

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16
Q

Insulin

A

produced by B cells of islets of langerhans in pancreas, tyrosine kinase receptors in liver, adipose and skeletal muscle

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17
Q

Glucagon-like peptide-1 (GLP-1) receptor agonists

A

incretin hormone (Gs), enhances glucose-mediated insulin secretion, peptide drugs with different half lives, subcutaneous. control food intake

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18
Q

Dipeptidyl peptidase 4 (DDP-4)

A

cleaves dipeptide from N terminal of GLP1 and GIP incretin, orally

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19
Q

Obesity

A

can lead to cancer, atherosclerosis, socioeconomic. Genetics, sedentary lifestyle, calories, environmental obesogens

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20
Q

Obesity pharmacology

A

block nutrient absorption, neuroactive compounds->appetite centres, block natural endogenous hormones

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21
Q

Amylin receptor agonists

A

37 aa peptide hormone produced by pancreatic b cells ->blood glucose, Gas receptors in brain.

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22
Q

Cardiovascular disease

A

(atherosclerosis, thrombosis, haemorrhage) ischaemic heart disease-blood clot in coronary arteries (angina-fatty material in artery/heart attack)

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23
Q

Hypertension

A

high blood pressure, increases risk. Below 140/90 = normal, 160/100 = treatment. -> cardiac hypertrophy, arrythmia, heart attack

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24
Q

Hypertension drugs

A

diuretics, b-blockers, calcium channel blockers, ACE inhibitors, a1 blockers (long term controlled by kidneys (RAA system))

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25
Q

B-blockers

A

block B1 in heart, decrease heart rate and force of contraction, only when sympathetic system activated.

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26
Q

a blockers

A

non specific- symp+CNS effects (a2 NA release), a1 blockers- reduced cardiovascular resistance, not first choice

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27
Q

Cannabis

A

tolerance example-CB1 receptors internalised, withdrawal (eat less food, sleep less),

28
Q

Methadone

A

substitution therapy for opioids, long half life

29
Q

antagonist therapy for opioids

A

Naltrexone, u, S and k

30
Q

Disulphram

A

punishment therapy for opioids

31
Q

Amphetamines

A

methamphetamine (NE+D), methyphenidate, methylenedioxymethamphetamine (S+NE)

32
Q

MDA

A

toxic metabolite of MDMA (shown more in rats than humans)

33
Q

asprin

A

COX inhibitors (non-specific) - acetylsalicylic acid, irreversible binds to SER, PGE2 PGL2, TXA2-decrease platelet aggregation

34
Q

ibuprofen

A

COX inhibitors (non-specific) - reversible, fewer adverse effects

35
Q

Diclofenac

A

COX inhibitor, (voltaren), lower doses, side effects-GI + headaches.

36
Q

Paracetamol

A

COX1/2 weak, analgesic + antipyretic, no GI effects. Can cause kidney damage/hepatoxicity

37
Q

COX 2 inhibitor example

A

celecoxib, etoricoxib (celebrex), anti imflam without COX1-GI effects

38
Q

Morphine

A

oral, 15-60 min onset, 3-6 hour duration, first pass metabolism (pain, laboured breathing, severe cough, diarrhea)

39
Q

fentanyl

A

high efficacy (8- times more potent than morphine), oral (10-15 min onset, 1-2 hours duration)+ transdermal (12-17 hours, 72 hours), lipophilic

40
Q

Tramadol

A

acts on u receptors and NA reuptake, decreased risk of respiratory depression + dependance

41
Q

Migraine prevention

A

propranolol, atenolol, amitriptyline, topiramate

42
Q

Triptan examples

A

sumatriptan, rizatriptan, eletriptan (side ffects- burning, tingling of face+ contraindicated with cardiovascular disease)

43
Q

Ditan examples

A

lasmiditan

44
Q

Anti-CGRP

A

rimegepart, ubrogepa (oral +acute small molecule receptor antagonist), eptinezumab (intravenous), erenumab, fremanezumab, galcanezumab (subcutaneous+antiCGRP receptor mAb antagonist )

45
Q

Diabetes treatments

A

biguanides, sulfonylureas, thiazolidinediones, SGLT2 inhibitors, DPP4 inhibitors, GLP1 agonists, insulins

46
Q

GLP-1 receptor agonist examples

A

exenatide, dulaglutide, semaglutide, liraglutide (obesity)

47
Q

DPP-4 comp inhibitor examples

A

vildagliptin, sitagliptin, saxaglipton

48
Q

Amyline agonists

A

Pramlintide - 3 aa changes -> no aggregation, half life 26-50 min, 3 x day injection
Cagrilintide - long acting (use with semaglutide)

49
Q

Metoprolol tartrate

A

oral, complete absorption, half life-3-4 hours, dose-20-200 mg daily (also used in congestive heart failure)

50
Q

Asthma

A

hyper-responsive to air + inflammation + mucus + bronchoconstriction

51
Q

Corticosteroids

A

mimics cortisol, nuclear receptor (takes time) reduce inflammatory effects, vascular permeability, no effect on bronchodilation, cant reverse remodelling.

52
Q

Steroid side effects

A

cushings syndrome, reduced via inhalation (10% lung, 90% swallowed, 1% systemic circulation), oral for acute attacks - high dose short course

53
Q

Leukotriene receptor antagonists

A

GPCR, influence cell function - airway muscle constriction, vascular permeability, increased chemotaxis. Less potent, reduced ADR

54
Q

SABA

A

short acting beta agonist - relievers. several hours + quick, beta 2 selective, relax airways, reduce bronchoconstriction/mucus, as required

55
Q

LABA

A

long acting beta agonist - controllers, long term bronchodilation, long lipophilic side chain-resist degradation, doesn’t address inflammation

56
Q

Muscarinic receptor blockers

A

asthma reliever-decrease bronchial tone, given with b2 agonist, slight chance of side effects

57
Q

Methylxanthines

A

second line controller, blocks cAMP (bronchodilation) ->AMP, adenosine receptor inhibitor (bronchial tone)

58
Q

Asthma corticosteroid preventers

A

Fluticasone - inhaled corticosteroid, first pass metabolised
Prednisolone- liquid oral corticosteroid
Prednisone - tablet oral corticosteroid

59
Q

leukotriene comp antagonists

A

Montelukast, zafirlukast (preventer)

60
Q

inhibitor of 5-lipoxygenase

A

Zileuton - prevents leukotriene formation (preventer)

61
Q

SABA example

A

Salbutamol - 10-25 min onset, 2-5 hour duration, adrenaline analogue (tremor, increase heart rate and force, decrease bp -> tachycardia)

62
Q

muscarinic receptor antagonist example (asthma)

A

Ipratropium, 30 min onset, 3-5 hour duration

63
Q

methylxanthine example

A

Theophylline - 2 hour onset, 8.5 hour half life, narrow therapeutic range

64
Q

Asthma controller example

A

Salmeterol/formoterol - LABA, twice a day, given with corticosteroids, peak effect 1-2 hours, 12-24 h duration.

65
Q

Relapse prevention

A

substitution therapy (agonist), antagonist therapy, punishment therapy

66
Q

Pancreatic lipase inhibitor

A

Orlistat - blocks nutrient absorption (faecal incompetence, GI upset, fat soluble vitamin deficiency)

67
Q

Compound that acts on brain appetite centres

A

Phentermine, topiramate, lorcaserin - POMC neuron activator (dry mouth, insomnia, headache, dizziness)

PHAL211 (5 decks)

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