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PHAL211 > Drugs > Flashcards

Drugs Flashcards

(67 cards)

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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
B-blockers
block B1 in heart, decrease heart rate and force of contraction, only when sympathetic system activated.
26
a blockers
non specific- symp+CNS effects (a2 NA release), a1 blockers- reduced cardiovascular resistance, not first choice
27
Cannabis
tolerance example-CB1 receptors internalised, withdrawal (eat less food, sleep less),
28
Methadone
substitution therapy for opioids, long half life
29
antagonist therapy for opioids
Naltrexone, u, S and k
30
Disulphram
punishment therapy for opioids
31
Amphetamines
methamphetamine (NE+D), methyphenidate, methylenedioxymethamphetamine (S+NE)
32
MDA
toxic metabolite of MDMA (shown more in rats than humans)
33
asprin
COX inhibitors (non-specific) - acetylsalicylic acid, irreversible binds to SER, PGE2 PGL2, TXA2-decrease platelet aggregation
34
ibuprofen
COX inhibitors (non-specific) - reversible, fewer adverse effects
35
Diclofenac
COX inhibitor, (voltaren), lower doses, side effects-GI + headaches.
36
Paracetamol
COX1/2 weak, analgesic + antipyretic, no GI effects. Can cause kidney damage/hepatoxicity
37
COX 2 inhibitor example
celecoxib, etoricoxib (celebrex), anti imflam without COX1-GI effects
38
Morphine
oral, 15-60 min onset, 3-6 hour duration, first pass metabolism (pain, laboured breathing, severe cough, diarrhea)
39
fentanyl
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
Tramadol
acts on u receptors and NA reuptake, decreased risk of respiratory depression + dependance
41
Migraine prevention
propranolol, atenolol, amitriptyline, topiramate
42
Triptan examples
sumatriptan, rizatriptan, eletriptan (side ffects- burning, tingling of face+ contraindicated with cardiovascular disease)
43
Ditan examples
lasmiditan
44
Anti-CGRP
rimegepart, ubrogepa (oral +acute small molecule receptor antagonist), eptinezumab (intravenous), erenumab, fremanezumab, galcanezumab (subcutaneous+antiCGRP receptor mAb antagonist )
45
Diabetes treatments
biguanides, sulfonylureas, thiazolidinediones, SGLT2 inhibitors, DPP4 inhibitors, GLP1 agonists, insulins
46
GLP-1 receptor agonist examples
exenatide, dulaglutide, semaglutide, liraglutide (obesity)
47
DPP-4 comp inhibitor examples
vildagliptin, sitagliptin, saxaglipton
48
Amyline agonists
Pramlintide - 3 aa changes -> no aggregation, half life 26-50 min, 3 x day injection Cagrilintide - long acting (use with semaglutide)
49
Metoprolol tartrate
oral, complete absorption, half life-3-4 hours, dose-20-200 mg daily (also used in congestive heart failure)
50
Asthma
hyper-responsive to air + inflammation + mucus + bronchoconstriction
51
Corticosteroids
mimics cortisol, nuclear receptor (takes time) reduce inflammatory effects, vascular permeability, no effect on bronchodilation, cant reverse remodelling.
52
Steroid side effects
cushings syndrome, reduced via inhalation (10% lung, 90% swallowed, 1% systemic circulation), oral for acute attacks - high dose short course
53
Leukotriene receptor antagonists
GPCR, influence cell function - airway muscle constriction, vascular permeability, increased chemotaxis. Less potent, reduced ADR
54
SABA
short acting beta agonist - relievers. several hours + quick, beta 2 selective, relax airways, reduce bronchoconstriction/mucus, as required
55
LABA
long acting beta agonist - controllers, long term bronchodilation, long lipophilic side chain-resist degradation, doesn’t address inflammation
56
Muscarinic receptor blockers
asthma reliever-decrease bronchial tone, given with b2 agonist, slight chance of side effects
57
Methylxanthines
second line controller, blocks cAMP (bronchodilation) ->AMP, adenosine receptor inhibitor (bronchial tone)
58
Asthma corticosteroid preventers
Fluticasone - inhaled corticosteroid, first pass metabolised Prednisolone- liquid oral corticosteroid Prednisone - tablet oral corticosteroid
59
leukotriene comp antagonists
Montelukast, zafirlukast (preventer)
60
inhibitor of 5-lipoxygenase
Zileuton - prevents leukotriene formation (preventer)
61
SABA example
Salbutamol - 10-25 min onset, 2-5 hour duration, adrenaline analogue (tremor, increase heart rate and force, decrease bp -> tachycardia)
62
muscarinic receptor antagonist example (asthma)
Ipratropium, 30 min onset, 3-5 hour duration
63
methylxanthine example
Theophylline - 2 hour onset, 8.5 hour half life, narrow therapeutic range
64
Asthma controller example
Salmeterol/formoterol - LABA, twice a day, given with corticosteroids, peak effect 1-2 hours, 12-24 h duration.
65
Relapse prevention
substitution therapy (agonist), antagonist therapy, punishment therapy
66
Pancreatic lipase inhibitor
Orlistat - blocks nutrient absorption (faecal incompetence, GI upset, fat soluble vitamin deficiency)
67
Compound that acts on brain appetite centres
Phentermine, topiramate, lorcaserin - POMC neuron activator (dry mouth, insomnia, headache, dizziness)

PHAL211 (5 decks)

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