Pharmacology Flashcards by Sereen Feroz

Name the routes of administration

Enteral - through GIT
Oral (PO), rectal (PR)

Parenteral - non GIT
SC
IM
IV
Sublingual
Inhalers (INH)

Local effect
Transdermal e.g. patches
Topical cream e.g. steroid

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Define agonist

Full affinity and full efficacy
∴ ↑ activation of receptor

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Define antagonist

Full affinity and zero efficacy
∴ ↓ activation of receptor

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Define affinity

How well ligand bind to receptor

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Define efficacy

How well a ligand successfully activates its receptor

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Define potency

The relative strength of drug
i.e. lower dose needed for response = more potent

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Describe the mechanism of a competitive inhibitor

Binds at the active site
∴ ↓ Efficacy
Reversible, affinity is unchanged
∴ Less potent

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Describe the mechanism of a non-competitive inhibitor

Binds away from active site, changing its shape
∴ ↓ Efficacy
Irreversible, affinity is reduced
∴ Less potent

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Define bioavailability

How much drug is uptaken systemically for effect
IV route = always 100%
Other routes = suboptimal

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What is a therapeutic range?

Upper and lower of safe doses of a drug
Narrowe range = reqs more care in dispensing

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Name some drug targets and examples of each

Receptor action - ARBs, BBs, salbutamol, tamoxifen, alpha blockers
Enzymes - ACEi, 5-alpha reductase inhibitors
Ion channels - CCB
Transporters - PPI

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Define pharmocodynamics

Effect of drug on the body

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Define pharmacokinetics

Effect of body on the drug
(when it’s being broken down)

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State the 4 aspects of Pharmacokinetics

ADME

Administration (route)
Distribution
Metabolism! (IV skips this!)
Excretion (hepatically or renally)

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Describe GIT metabolism

Mechanical and chemical digestion

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Describe renal metabolism

Simple, already soluble molecules. Easy to pee out directly

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Describe hepatic metabolism

More complex, hydrophobic molecules. Undergo phase 1 and/or phase 2 reacns

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Describe Phase 1 reactions

NON-conjugation. Aims to slightly increase hydrophilicity.
By microsomal enzymes e.g. CYP450

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Descrive Phase 2 reactions

Conjugation. Adds functional groups
e.g. glucuronidation to massively increase hydrophilicity

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Name the 2 main receptors of cholinergic pharm

Nicotinic and muscarinic

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Describe Nicotinic receptors

Usually pre-synpatic

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Describe Muscarinic receptors

Usually post-synaptic

M1 = BRAIN
M2 = HEART
M3 = LUNGS

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What condition is related to disrupted Ach Transmission at NMJ?

Myasthenia Gravis

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Side/Effects of XS acetylcholine stimulation

SLUDGE

Salivation
Lacrimation
Urination
Defecation
GI distress
Emesis

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Name the receptors of adrenergic pharm

alpha 1 & 2 beta 1 beta 2

Where are alpha 1 & 2 found?

On vessels and sphincters (e.g. bladder neck)

Example of alpha 1 block and its use + mechanism

Tamsulosin 1st line med for BPH Relaxes bladder neck ∴ easier urine flow

Where is beta 1 found?

On heart

Give an example of a beta 1 agonist and its use + mechanism

e.g. Dobutamine - Cardiogenic shock, increases force and rate of cardiac contraction

Give an example of a beta 1 antagonist and its use + mechanism

Beta blockers - decrease force and rate of cardiac contraction

Another word for force of contraction

Inotropy

Another word for rate of contraction

Chronotropy

When are BBs CI?

ASTHMA

Where are beta 2 receptors found?

On lungs

What does a beta 2 agonist do?

Bronchodilation of airways SABA !!

What are beta blockers known as and why?

Cardioselective drugs Mostly act on cardiac tissue ∴ beta 1 only blockers prescribed

State the types of adverse drug reactions

**A**ugmented (common) **B**izarre **C**hronic use **D**elayed **E**nd of use

What should you do if you witness an adverse drug reaction?

Report to MHRA! Using Yellow card scheme!!

What is the bioavailability of opioids?

50%

Generally, when do you use opioids?

For chronic severe pain usually cancer pain

5mg diamorphine is equivalent to

10 mg morphine = 100 mg pethidine

Main SE of opiate use?

Constipation

How do you treat an opiate overdose?

IV Naloxone

Complications of paracetamol overdose

Fulminant liver failure Shutdown of basic physiological systems e.g. shock Can lead to death!

How is paracetamol metabolised? (check)

Hepatic metabolism Phase 2 - 95% Phase 1 - 5%

Describe the pathophysiology behind a paracetamol overdose

Phase 2 pathway gets overwhelmed ∴ increase of Phase 1 pathway This route includes production of **NAPQI** = hepatotoxic !! ∴ ↑ Phase 1 metabolism = ↑ NAPQI ∴ Liver failure !!

DOAC mechanism and examples

Inhibits factor 10a Apixaban, Rivaroxaban

Warfarin mechanism

Inhibits 10, 9, 7, 2 (1972 - Vit K dependent factors)

LMWH mechanism

Inhibits 10 and thrombin

Alteplase (IV) mechanism

Fibrinolytic. Essentially tPa - activates plasmin to eat fibrin mesh

Antiplatelet mechanism and examples

Inhibits P2Y12 - affects primary platelet plug Clopidogrel, ticagrelor

NSAIDs mechanism

Inhibits arachidonic acid pathway Cox-1 and Cox-2

Cox-1 role and s/e of its inhibition

Involved in prostaglandin synthesis, protects gastric mucosa Peptic ulcer!!

Describe Cox-2 pathway

Targeted pathway Activation of Cox-2 is involved in inflammation

Example of selective Cox-2 inhibitor

Celecoxib

Mechanism of Loop Diuretic

Acts on ascending limb of loop, inhibits NKCC2 channels

Example of Loop Diuretic

Furosemide

Mechanism of thiazide diuretic

Acts on DCT, inhibits Na-Cl co-transporter

Example of thiazide diuretic

Bendroflumethiazide

Mechanism of aldosterone antagonist

K+ sparing diuretic, acts on aldosterone receptors of collecting duct Increases Na+ excretion and retains K+

Example of aldosterone antagonist

Spironolactone

Give examples of anti-hypertensives

ACEi - ramipril CCB - amlodopine, verapamil

What do PPIs do and give an example

Reduces acidity of GI lumen e.g. Lanzoprazole

Main S/E of ACEi Why does this happen?

Dry cough Build up of bradykinin

Difference between tolerance and dependence

Tolerance = Physiological Dependence = Psychological

Main S/E of CCB What condition is this sometimes mistaken for?

Ankle swelling Heart failure!

1st Line treatment for anaphylaxis

Adrenaline, 500 mcg, IM

Prophylaxis for MI

**ACAAB** ACEi (maintain BP) CCB (BP) Aspirin Atorvastatin BB (reduce HR to prevent shearing of coronary arteries)

Acute Tx for MI

**MONAC** Morphine, Oxygen (IF NEEDED), Nitrates, Aspirin, clopidogrel

1st line Tx for T2DM Why? Main S/E

Biguanide - **Metformin** Increases peripheral tissue sensitivity to insulin GI distress and stomach pain

Pharmacology Flashcards

(70 cards)