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Drugs Term 1 > Drug term 1 > Flashcards

Drug term 1 Flashcards

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1
Q

Atracurium

A

NMB, competitive antagonist for nAChR, intubation, abdominal surgery, therapeutic hypothermia

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2
Q

Doxazosin

A

alpha 1- adrenoceptor antagonist, Pheochromocytoma surgery, Benign Prostatic Hyperplasia (urethral blockage)

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3
Q

Gefitinib

A

TK inhibitor for Lung Cancer (competes for ATP at EGFR)

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4
Q

Cetuximab

A

monoclonal antibody, prevents ligand binding at EGFR for Colorectal Cancer

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5
Q

Beclametasone

A

anti-inflammatory glucocorticoid (for severe asthma), reduces cytokines, increases annexin 1, reduces mast cell degranulation

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6
Q

Tamoxifen

A

competitive antagonist for ER in Breast Cancer

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7
Q

Quinidine

A

P-gp inhibitor

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8
Q

Loperamide

A

treats diarrhoea in gastroenteritis, acts on µ-opioid receptors

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9
Q

Quinidine + Loperamide

A

Loperamide passes through BBB, produces central morphine-like effects

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10
Q

Ranitidine

A

Histamine2 Receptor Antagonist, reduces gastric acid production

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11
Q

Gefitinib + Ranitidine

A

Gefitinib is a weak base (2nd and 3rd amine), 21mg/ml at pH1, <0.001mg/ml at pH7, pH-dependent aqueous solubility.
Ranitidine increases pH in GI tract, reduces Gefitinib solubility and F.
Before 250mg of Gefitinib dose, causes 44 and 70% reduction in AUC and Cmax

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12
Q

Dabigatran

A

anti-coagulant (direct thrombin inhibitor), substrate for P-gp

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13
Q

Ketoconazole

A

P-gp inhibitor

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14
Q

Dabigatran + Ketoconazole

A

increased peak Dabigatran concentration, causes a severe haemorrhage

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15
Q

Furanocoumarin

A

found in Grapefruit juice, CYP450 and P-gp inhibitor, discovered in clinical trial of Felodipine (anti-hypertensive) taken with ethanol. Increased F and AUC

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16
Q

L-Dopa

A

prodrug for Dopamine, substrate for SLC7A5 and transport across BBB in Parkinson’s treatment

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17
Q

Acyclovir and Valacyclovir

A

treatment for Herpes, Acyclovir Foral = ca. 15%, Valacyclovir Foral = ca. 60%, Valacyclovir is a good substrate for SLC15A1 (PEPT1) = symport with H+

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18
Q

Codeine

A

converted to morphine by CYP2D6 via O-dealkylation, in Ultra Rapid Metabolisers can cause respiratory depression in days

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19
Q

Warfarin

A

anticoagulant, aromatic hydroxylation at many points by CYP450 depends on isomer (S-isomer more potent),
can cause Type A reactions

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20
Q

Warfarin + Fluconazole

A

inhibition of CYP2C9, less S-isomer Warfarin metabolism, causes haemorrhage

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21
Q

Fluconazole

A

treatment for oral thrush, inhibits CYP2C9

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22
Q

Phenytoin

A

hydroxylation by CYP2C9 to hydroxy-phenytoin

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23
Q

Paracetamol Overdose

A

converted to non toxic metabolites via glucuronidation and sulfation.
highly reactive NAPQI also produced by N-hydroxylation, hepatocellular supply of Glutathione for conjugation is depleted, reacts with cellular membrane molecules causing hepatocyte damage

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24
Q

St John’s Wort

A

herbal medicine for mental health, CYP3A5 and CYP3A4 inducer, increases metabolism of active components in oral contraceptives

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25
Cidofovir
acyclic nucleoside analogue, treats cytomegalovirus infections, OAT-mediated accumulation in proximal tubule cells of kidney, dose-limiting toxicity
26
Probenecid
treats gout and hyperuricaemia, inhibitor of OAT
27
Cidofovir + Probenecid
Probenecid acts as a nephroprotectant
28
Digoxin + Quinidine
cardiac glycoside for heart failure and atrial fibrillation, small therapeutic window, administered with Quinidine = dangerous levels
29
Phenoxymethylpenicillin
taken on empty stomach, gastric acid causes chemical degradation
30
Saquinavir
antiretroviral for AIDS/HIV treatment, very hydrophobic, taken with high fat meal for dissolution and bile emulsifies fats
31
Tetracycline
not to be taken with food, forms insoluble chelates with Fe and Ca (MILK)
32
Gentamicin
antibody, IV treatment for Sepsis, polar drug with narrow therapeutic window. Will distribute into fat, will not into extracellular fluid accumulation (systemic oedema)
33
Digoxin
cardiac glycoside administered by IV loading. Fu = 0.9 but highly bound in cardiac tissue. V reduced in renal disease as metabolites not efficiently excreted and can displace Digoxin from tissues. V calculated using eGFR or CLcr
34
Venlafaxine
SSRI = antidepressant t1/2 ca. = 5hr, often causes discontinuation syndrome
35
Fluoxetine
SSRI = t1/2 ca. = 48-72hr, low risk of discontinuation syndrome
36
N-acetyl cysteine (NAC)
treatment for Paracetamol Overdose, precursor for glutathione via IV infusion. Can bind to NAPQI and neutralise it
37
Glycerl Trinitrate
for angina, administration sublingually (rapid onset of action)
38
Afrezza
rapid-acting inhaled insulin for diabetes
39
Adalimumab
anti-inflammatory, anti-TNFα, via SC injection, cytokine inhibitor
40
Fentanyl
rapid buccal absorption formulation
41
Buprenorphine
for opioid drug dependence, prolonged buccal formulation
42
Midazolam
rescue medicine (buccal) to manage a seizure
43
Vitamin A
low dose = blindness, high dose = loss in bone density, cognitive problems, death
44
Tropicamide
non-selective muscarinic antagonist, Mydriasis, Cycloplegia, paralysis = no reaction to light, for eye exams
45
Tetracaine
local anaesthetic, blocks VGSCs, reduces Corneal Reflex
46
Phenylephrine
α1-adrenoceptor agonist, Mydriasis, reduction in Sclera redness (vasoconstrictive), reaction to light reduced
47
Pilocarpine
non-selective muscarinic agonist, Miosis, treatment for Closed Angle Glaucoma
48
Timolol
non-selective β-adrenergic antagonist (beta blocker), treatment for Open Angle Glaucoma (reduces humour production and IOP)
49
Ephedrine
non-selective adrenoceptor agonist, treats hypotension. Resistant to COMT (no OH groups at 3 & 4) reduces potency but increases F, MAO (CH3 group at αcarbon) blocks oxidation. Flips NA transporter easily converted to Methamphetamines, used to be found in Sudafed
50
Tyramine
found in wine and cheese, flips NA transport
51
Tyramine + MAO inhibitor
MAO inhibitor for depression and Parkinson's, Tyramine not metabolised causes a hypertensive crisis
52
Amphetamine
flips NA transporter, promotes NA release from vesicles via VMAT. also acts at DAT and SERT
53
Methamphetamines
stronger effect than Amphetamines
54
Cocaine
high affinity and inhibits NET, DAT and SERT, blocks VGSCs (local anaesthetic)
55
Botulinum Toxin (Botox)
inhibits ACh release by cleaving SNARE proteins from plasma membrane and vesicles. treatment for Overactive Bladder Syndrome (injections in detrusor muscle), relaxes facial muscles, treats hyperhidrosis
56
Novichock
AChEi, organophosphate (Russian nerve agent), causes DUMBELLSS, coma and suffocation. Non-competitive inhibition. treated with Atropine (muscarinic antagonist) and Hagedorn Oxime (Pralidoxime) to reactivate AChEi
57
Tubocurarine
competitive antagonist for nAChR, very big molecule (can't permeate membranes), paralysis
58
Neostigmine
AChE inhibitor, treatment for Tubocurarine poisoning and Myasthenia Gravis (chronic autoimmune disease, skeletal muscle weakness in the face)
59
Atropine
muscarinic antagonist from Belladonna, causes Mydriasis, increased IOP and blindness. treatment for Bradycardia, blocks ACh from vagus nerve
60
Tetrodotoxin
inhibits VGSCs, heat-stable from puffer fish. Causes diaphragm and intercostal muscle paralysis, leading to respiratory failure
61
Bupivacaine
long-acting local anaesthetic
62
Lignocaine
short-acting local anaesthetic
63
Acetyl-α-Methylcholine
CH3 substituted at αCarbon, increases nicotinic potency
64
Acetyl-β-Methylcholine
CH3 substituted at βCarbon, increases muscarinic potency
65
Carbachol
acyloxy group replaced with NH3, resistant to AChE, treatment for Closed Angle Glaucoma
66
Bethanechol
CH3 substituted at βCarbon, acyloxy group replaced with NH3, muscarinic potent and resistant to AChE
67
Isoprenaline
β1 and β2 selective, due to large terminal substitutions, more N-methylated than Adrenaline
68
Salbutamol
β2 selective, due to large terminal substitutions and 3'-hydroxymethyl and 4'-hydroxy substitutions
69
Adrenaline
more β potent than Noradrenaline
70
Captopril
ACE inhibitor, antihypertensive (competitive antagonist), reduces Angiotensin II and Aldosterone release from Teprotide from Brazilian Viper venom
71
Thalidomide
Optical Isomers: R = desired sedative and anti-inflammatory effects S = teratogenic effects liver interchangeably converts them
72
Pentobarbitone
short-acting sedation (positional isomers)
73
Amobarbitone
long-acting sedation (positional isomers)
74
Antihistamines
inverse agonists for H receptors (GPCRs) 1st generation can pass through BBB (not P-gp substrate)
75
Penicillin
Type B reaction, anaphylaxis
76
Biphosphonates
Type C reaction, osteonecrosis of jaw
77
Lomustine
Type D reaction, Leucopoenia up to 6 weeks after dose
78
Benzodiazepines
Type E reaction, withdrawal causes insomnia and anxiety

Drugs Term 1 (1 decks)

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