Pharm Flashcards by Galvin Chiam

Diabetes drugs

Metformin
DPP-4 inhibitors(sitagliptin)
Sulphonylurea(gliclazide)
SGLT-2 inhibitors(dapaglifozin)

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Metformin action

Activates AMP kinase in heaptocyte mitochondria

Inhibit ATP production->inhibit gluconeogenesis

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Metformin side effects and absorption/distribution

GI problems

Metformin requires OCT-1 to be absorbed
Found in liver, kidney, bowel

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DPP-4 inhibitor action and side effects

Inhibit DPP4 in vascular endothelium and metabolises incretin in plasma
Insulin production secreted
Incretins also slow digestion/cut appetite

URTI- flu like symptoms

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Sulphonylurea action and side effects

Inhibits ATP dependent K channel in pancreatic beta cell
Depolarisation->insulin exocytosis

Weight gain
Hypoglycaemia

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SGLT-2 inhibitor action and side effects

Reversibly binds to SGLT-2 in PCT
Reduce glucose reabsorption
Helps with albuminuria in CKD
Efficacy depends on renal function

UTI

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Metformin adjustment based on eGFR

> 60 -> none
45-60 -> 3-6month monitoring
30-45 -> 50% decrease
<30 -> contraindicated

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Epilepsy drugs

Lamotrigine
Levetiracetam
Sodium valproate
Diazepam

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Lamotrigine action and side effects

Blocks VGSC->precent Na influx
Prevent depolarisation in glutamatergic neurons

Rash
Drowsiness
SJSTEN(uncommon)
Suicidal thoughts(uncommone)

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Levetiracetam action and side effects

Inhibit synaptic vesicle protein SV2A
Prevent glutamate exocytosis

Fatigue
Headache
Dizziness

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Sodium valproate action and side effects

Inhibit GABA transaminase->prevent GABA breakdown

Stomach pain
Diarrhoea
Drowsiness
Weight gain

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Antiepileptic not used for pregnant women

Sodium valproate

Neural tube defects
Decreased IQ
Autism

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Diazepam action and side effects

Binds to benzodiazepine binding site on GABA-A receptor
Increase chloride influx when GABA bind
Hyperpolarisation

Drowsiness
Respiratory depression

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Depression drugs

Citalopram
Sertraline
Fluoxetine
Venlafaxine
Mirtazapine

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SSRIs drugs and side effects

Citalopram, sertraline, fluoxetine

GI problems
Sexual dysfunction
Anxiety
Insomnia
Citalopram: M & H1 receptor antagonist
Sertraline: inhibit DA transporter
Fluoxetine: HT2A&HT2C R antagonist

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Venlafaxine action and side effects

SSRI
Also inhibit noradrenaline reuptake

SSRI side effects
Hypertension

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Mirtazapine action and side effects

5HT-2 and alpha 2 receptor antagonist-> 5HT-1R unopposed->antidepressant
Histamine H1 receptor antagonist->sedation

Weight gain
Sedation

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Antidepressants that prolong QT interval

Citalopram

Venlafaxine

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Hypertension drugs

ACEi: ramipril, lisinopril
ARBs: losartan
CCBs: amlodipine
Thiazine diuretics: indapamide

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ACEi action and side effects

Inhibit AT2 production
Vasodilation and less aldosterone

Cough(bradykinin)
Hyperkalaemia(efferent arteriole vasoD)
Foetal injury
Renal injury

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Calcium channel blockers action and side effects

Block L type CC in vascular smooth muscle
Lower Ca influx
Heart pumps less strongly
Peripheral vessel vasodilation

Ankle oedema
Constipation
Palpitations
Flushing/headache

Thiazide/thiazide-like diuretics action and side effects

Block Na-Cl cotransporter in DCT
Less water reabsorbed

Hypokalaemia
Hyponatraemia
Metabolic alkalosis(high H secretion)
Hypercalcaemia
Hyperuricaemia

ARBs action and side effects

Non-competitive antagonist at AT-1 receptor in kidneys & vasculature

Hypotension
Hyperkalaemia
Foetal injury
Renal failure
Not as effective as ACEi

Stages of hypertension

Under 135/85: 5 year monitoring
149/94: drugs if comorbidities
Above: start drugs

Antihypertensive used for african/caribbean people

ARBs

Asthma drugs

Salbutamol Steroids: fluticasone, mometasone, budesonide Montelukast

Salbutamol action and side effects

Beta 2 adrenergic receptor agonist on airway smooth muscle Prevents smooth muscle contraction Palpitations Tachycardia/arrhythmia Hypokalaemia at higher doses

Salbutamol features(half life etc)

SABA 2.5-5h half life Not absolutely selective

Asthma steroids action and side effects

Decreases immune cells and cytokines Higher affinity for glucocorticoid receptor than cortisol Lower IL-5 secretion ``` Sore throat Opportunistic infection Growth retardation Hyperglycaemia Low bone density Immunosuppression ```

Asthma steroid oral bioavailability and efficacy

Fluticasone and mometasone: <1% Budesonide: >10% ->some GI absorption Budesonide not as potent

Montelukast action and side effects

CysLT-1 leukotriene receptor antagonist Lower eosinophil migration Less bronchoconstriction Less inflammatory oedema Diarrhoea Fever Headache Nausea/vomiting

When to administer montelukast

2 hours before exercise->prophylaxis of exercise induced bronchoconstriction

Analgesic drugs

NSAIDs: ibuprofen, naproxen, diclofenac Paracetamol Aspirin Opioids

NSAID action and side effects

Inhibit COX->inhibit prostanoid production->anti-inflammation Prostanoid(prostaglandin, thromboxane) COX-2 inhibition->analgesia, antipyretic ``` Gastric ulceration(COX-1 inhibition) Rash, dizziness, tinnitus Chronic renal failure(prolonged use) ```

Paracetamol action and side effects

Inhibit peroxidase, mild COX inhibition Not anti-inflammatory Analgesic, antipyretic Skin reaction Hepatotoxicity if overdose

Dyspepsia drugs

PPIs: omeprazole, lansoprazole | H2 receptor antagonist: ranitidine

PPI action and side effects

Irreversible inhibition of H/K ATPase in parietal cells Single dose lowers secretions by 90% ``` Osteoporosis due to high pH(Ca) Headache Diarrhoea Bloating Abdominal pain Rashes ```

Histamine H2 receptor antagonist action and side effects

Competitive antagonist on parietal cell Inhibit gastric secretions by 60%->twice daily dose Diarrhoea Dizziness Muscle pain Transient rash

Aspirin action and side effects

Inhibit COX->prevent oxidation of arachidonic acid->low thromboxane A2-> low platelet aggregation Low PGE2->reduced pain, sensation and fever Dyspepsia Haemorrhage

Statin action and side effects

HMG-CoA reductase inhibitor Cholesterol synthesis inhibited(liver) LDL uptake by liver Muscle toxicity Constipation Diarrhoea

What to monitor when administering statin

Hyperkalaemia | Acute renal failure

Trimethoprim action and side effects

Competitive inhibitor of dihydrofolate reductase Prevent purine synthesis for DNA and protein production Diarrhoea Skin reaction

Gentamicin action and side effects

Aminoglycoside Binds to 30s ribosomal subunit->prevent translation Ineffective against anaerobic bacteria Ototoxicity Nephrotoxicity

Drug that affects eGFR measurement

Trimethoprim inhibits active secretion of creatinine

Co-amoxiclav action and side effects

Binds to penicillin binding site Prevent transpeptidation Clavulanate inhibits beta lactamase Nausea Diarrhoea

Lactulose action and side effects

Non-absorbable disaccharide Retains water by osmosis Colonic bacteria metabolism increases laxative effect Abdominal pain Diarrhoea Flatulence Nausea

Weak and strong opioids

Weak: codeine, tramadol Strong: morphine, fentanyl

Opioids action and side effects

Depressant on cellular activity Activates opioid receptor Decreased perception of pain Nausea Vomiting Constipation

Opioid overdose symptom

Respiratory depression

Opioid effect on nociceptor pathway

Inhibits transduction at nociceptor Inhibits transmission at spinothalamic pathway Activates modulation on efferent tract