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Pharmacology Flashcards

1
Q

Type A Drug RXN

A

Related to pharmacodynamics of a drug

  • dose dependent and predictable
  • Known SE of meds
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2
Q

Type B Drug RXN

A

Unrelated to pharmacodynamics of drug

  • Unpredictable and mostly immunological
  • E.g. drug rash
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3
Q

Clearance units

A

L/min

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4
Q

1st order kinetics

A

same AMOUNT of drug eliminated per unit of time

Dependent on cencentration

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5
Q

Zero order kinetics

A

same PROPORTION of drug eliminated per unit of time

Independent of concentration

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6
Q

Dopamine MOA

A

D1 - Low doses - vasodilation
Beta 1 - Intermediate doses - Increase chronotropy (HR) and inotropy (SV)
alpha 1 - High doses - Vasoconstriction

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7
Q

Adrenaline/Noradrenaline MOA

A

Mostly Alpha 1 - vasoconstriction

Some Beta 1 and 2

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8
Q

Dobutamine MOA

A

Mostly Beta1 and Beta2

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9
Q

Neprolysin inhibitor MOA

A

• Inhibition of neprilysin (a neutral endopeptidase) raises levels of several endogenous vasoactive peptides, including natriuretic peptides, bradykinin, and adrenomedullin, and may thus have beneficial effects in patients with HF.

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10
Q

MOA Tranexamic acid

A

Inhibits breakdown of clots by blocking binding of plasminogen and plasmin to fibrin.

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11
Q

Elimination definition

A

Elimination refers to the irreversible removal of drug from the body by all routes of elimination

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12
Q

Clearance definition

A

Clearance may be defined as the volume of fluid cleared of drug from the body per unit of time

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13
Q

PTU MOA

A

Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine.

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14
Q

Carbimazole MOA

A

Carbimazole is a pro-drug as after absorption it is converted to the active form,methimazole. Methimazole prevents thyroid peroxidase enzyme from coupling and iodinating the tyrosine residues on thyroglobulin, hence reducing the production of the thyroid hormones T3 and T4

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15
Q

Potassium iodine MOA in Thyroid

A

iodine acutely inhibits hormonal secretion within hours [1], but the responsible mechanisms are uncertain.

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16
Q

MMF MOA

A

selectively suppresses lymphocyte proliferation and antibody formation by inhibiting inosine monophosphate dehydrogenase.

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17
Q

Which drug of abuse causes increased risk of seizures

A

Cocaine

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18
Q

Which OTC supp can cause hepatotoxicity

A

Valerian

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19
Q

achievement of steady state concentration is significantly delayed because this drug induces its own metabolism

A

CArbamazepine

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20
Q

Phase 0 Trial

A

To determine if drug engages its expected target

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21
Q

Phase 1 Trial

A

Initial safety check:

  • Determine safe dosage range
  • Identify SE and study toxicity profile
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22
Q

Phase 2 Trial

A

Explore efficacy while maintaining safety usually against placebo

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23
Q

Phase 3 Trial

A

Multiple dose trials and ascending dose trials

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24
Q

Phase 4 Trial

A

Trials after FDA approval

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25
Drugs that have zero order kinetics
ethanol, phenytoin and salicylates
26
why is morphine half life prolonged in renal failure
Impaired elimination of morphine-6-glucoronide
27
Alpha 1
Vasoconstriction
28
Beta 1
Increase in contractility of heart and HR
29
Beta 2
Vasodilation, bronchodilation
30
Dopaminergic
Vasodilation
31
MOA Red Man Syndrome with Vanc
NOT IgE mediated – is due to vancomycin directly activating mast cells resulting in release of vasoactive mediators (eg histamine)
32
Gold standard testing for allergic contact dermatitis
PAtch testing - as type 4 hypersensitivity reaction | Not prick or scratch testing - these are IgE mediated tests
33
PO Morphine to SC morphine PO Hydromorphone to SC Hydromorphone
2:1 or 3:1
34
PO Morphine to PO Codeine
1:10
35
PO Morphine to PO Hydromorphone
5:1
36
PO Morphine to PO Oxycodone
1.5:1
37
SC morphine to SC fentanyl
100:1
38
Phase 1 metabolism
introduction of a functional grouop (e.g. reduction, oxidation) – CYP450 has its place here
39
Phase 2 metabolism
conjugation of drug with large polar group to make it more hydrophilic (e.g. glucuronidation, sulphate conjugation)
40
Bioavailability
Defined as the fraction of unchanged drug reaching the systemic circulation following administration by any route
41
Bactrim side effects
o Hyperkalemia o Megaloblastic anaemia o Methaemoglobinemia
42
Mx of Tardive dyskinesia
Mild: Benzos Severe local: Botox injection Severe generalised: IV/ IM Benztropine 1-2 mg
43
Tx of Paracetamol overdose
1. Activated charcoal if presenting <4 hours 2. NAC if - Level above normogram after 4 hours - Unknown time of ingestion and level > 66 micromol/L - Any hepatotoxicity
44
What level of paracetamol level is there no risk of toxicity
if the paracetamol level is <120 μmol/L or 22 mg/L
45
Warfarin MOA
• The mechanism of warfarin is it INHIBITS the VKOR enzyme (thus inhibiting the reaction which makes oxidised vitamin K to reduced vitamin K, and therefore there is no vitamin K to act as a co-factor for the carboxylation of the coagulation factors to their active form)
46
WArfarin anticoagulant effect
Anticoagulants increase the time it takes for blood to clot  Blocking factors VII, IX and X is technically anticoagulation The ultimate anticoagulant effect of warfarin is delayed until the normal coagulation factors, especially prothrombin, are cleared from the circulation (plasma half life of prothrombin is ~3 days) This is why parental anticoagulants (LMWH, UFH) should overlap with warfarin for at least 4-5 days 
47
Warfarin antithrombotic effect
Antithrombotics reduce thrombus formation blocking factor II (thrombin) is antithrombotic
48
BEst benzos for elderly and cirrhotics and why
Lorazepam, oxazepam  and temazepam (“LOT”) metabolized by the liver through glucuronidation (Phase II not Phase I), which means § There are no active metabolites § These drugs are rarely susceptible to drug-drug interactions
49
When to give PJP prophylaxis with pred
PJP prophylaxis if >20mg prednisolone daily for >4wks 
50
Features of Aspirin OD
- Tachypnea (Direct stimulation of resp centre) - Usually Resp Alkalosis or mixed acidosis - Hypovolemia - LFT derrangement (increased lactate)
51
Mx of Aspirin OD
- Serum levels every 2 hours till peak (>7.2 = haemodialysis) - Avoid intubation - Fluid resus - MAINSTAY: Alkalinsation of serum and urine with HCO3 or HSAL
52
Features of NMS
Decreased GCS, Rigidity, dysautonomia, fever Elevated CK Occurs over days to weeks
53
Mx of NMS
``` Ventilation and fluids Cooling Antihypertensives Benzos for agitation CAse reports: Bromocriptine, amantadine, dantroline ```
54
Features of SS
Decreased GCS, MYOCONUS, HYPERREFLEXIA, dysautonomia, Fever Occurs over 24 hours
55
Mx of SS
Supportive care Sedation with benzos if needed Cyproheptadine (H1 antagonist)
56
Methadone SE
Orthostatic hypotension Long QTc Increased ICP
57
Dihydropyridines MOA
Peripheral CCBs | Bind to L type Ca channels on cells and prevent influx leading to vasodilation
58
Non-Dihydropyridines MOA
Central CCBs | Dialtes coronary arteries and decreases cardiac contractility and conduction
59
Clozapine MOA
• Antagonist at alpha, H1, cholinergic and other dopaminergic and serotonergic receptors
60
SE of Clozapine
○ Agranulocytosis, seizures, myocarditis, increased mortality in elderly, other CV effects (eg. Orthostatic hypotension) Risk of SEs is usually highest in early treatment course
61
Worst drug to cause lithium toxicity
Thiazides
62
LEvel at which Lithium Toxicity is seen
>1.5-2 mmol/L
63
SE of lithium
``` GIT Neurologic - Ataxia, dysarthria, tremors -Hypothyroid/Goitre -Sick sinus -QTc prolongation -Nephrogenic DI ```
64
Lithium Toxicity Treatment
Acute: Nil treatment usually needed, usually need chronic for uptake in brain Chronic: IV, possible dialysis
65
SSRI MOA
• SSRIs block the action of presynaptic serotonin reuptake pump 🡪 increases the amount of serotonin available in the synapse, increasing postsynaptic serotonin receptor occupancy.
66
SSRI SE
Sexual dysfunction Drowsiness Weight gain Anxiety/insomnia
67
Varenicline (Champix)
Partial agonist of nicotinic receptor § Concerns with psychiatric effects (eg. Risk of suicide in existing psych disease) and CV effects (small increased risk all CV events)
68
Bupropion (Zyban)
Enhances central NA and dopamine release § Also neuropsych concerns (also increased risk of suicide/self harm but possibly smaller risk than Champix)
69
Sympathomimetic Toxidrome
Tachycardia, hypertension, agitation, diaphoresis, hyperthermia (warm, wet skin) Cause: -Amphetamines, MAOIs, methylphenidate
70
Opioid toxidrome
Miosis, sedation, respiratory depression Tx: Naloxone
71
Cyanide poisoning Tx
Hydroxycobalamin
72
Benzo OD Tx
Flumazenil | -CI in seizures, benzo dependence
73
Iron OD Tx
Desferrioxamine | Whole bowel irrigation if lots of PO tablets on AXR
74
Organophosphate OD Tx
Atropine, Oximes
75
When is gastric lavage performed in OD
Only within one hour of ingestion of a life threatening OD | -E.g. >20 mg/Kg TCAs
76
When to consider whole bowel irrigation in OD
For iron, lithium, lead, and SR CCBs
77
Role for MDAC (Multi dose activated charcoal) in OD
Enhances elimination "GI Dialysis for drugs with entero hepatic recirculation" Carbamazepine, dapsone, colchicine
78
Toxic dose of paracetamol
200mg/kg or 10g, whichever is less
79
NAC SE and MX
Anaphylactoid reaction | -Stop infusion, antihistamine, and restart at half rate
80
When to continue NAC in paracetamol OD
ALT >50, INR >1.3, Paracetamol concentration >10mg/L, unwell patient
81
Quetiapine OD Features
CNS Depression Antcholingeric toxidrome Hypotension
82
Mx of Quetiapine OD
Supportive Alpha blocker - vasodilation IVF and Norad
83
SSRI Complications in OD
Hyperthermia is life threatening - Cyproheptadine is the antidote Citalopram/Escitalopram - QT prolongation/TdP
84
TCA OD Features
• Coma and tachycardia most common clinical features –present with 60-90 mins • Hypotension, seizures, ventricular arrhythmias • QRS prolongation, right axis deviation, upright R wave in AVR, PR prolongation
85
TCA OD MX
• Rx is IV Na bicarbonate 1-2 mmol/kg, repeated to pH 7.5—7.55 • Hyperventilate to maintain pH
86
Iron OD Features
haemorrhagic gastroenteritis: nausea, vomiting, haematemesis, metabolic acidosis, hypotension
87
Anticholinergic toxidrome Features
red as a beet, dry as a bone, blind as a bat, mad as a hatter, hot as a hare, and full as a flask flushing, dry skin and mucous membranes, mydriasis with loss of accommodation, altered mental status (AMS), fever, and urinary retention, respectively
88
Anticholinergic OD Tx
Activated charcoal IVF Physostigmine (reversible cholinesterase inhibitor)

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