Phase III drug list Flashcards

Question

**Nitrate Vasodilators**

Answer 1

* **Glycerol trinitrate (GTN)** * **isosorbide mononitrate (ISMN)** MOA: **NO release --\> Smooth muscle relaxation** * Metabolised to release Nitric Oxide (NO) which stimulates soluble *guanylate cyclase*. Increases *cGMP* in vasc. smooth muscle cells. Drives *dephosphorylation of MLC* via activation of *MLC Phosphatase* causing vascular smooth muscle relaxation. * *Heart Effects:* Can act to dilate arteries AND veins. Venodilation decreases preload. Coronary artery dilation increases blood and oxygen supply to the myocardium. Promote moderate arteriolar dilation- reduces cardiac afterload Use: **Acute angina pectoris, HF** SE: **Headache, Hypotension** Interactions: **Antihypertensives**

Answer 2

* **Noradrenaline (alpha)** * **Dobutamine (beta)** * **Adrenaline (alpha and beta)** * **Metraminol** * **Isoprenaline** MOA: **Adrenergic stimulation increased inotropy** * Positive inotrope: Binds & Stimulates Cardiomyocytes B₁ adrenergic receptor --\> Drives heart muscle contraction --\> Resotres function Uses: **Cardiac Arrest, Cardiogenic shock** SE: **Arrythmia** Interactions:-

Answer 3

**Aspirin** * **Inhibition of thromboxane synthesis** * Blocks enzyme actions of platelet COX enzyme. COX required for synthesis Thromboxane A2 production. Reduced TXA2 synthesis inhibits platelet activation & thrombus formation **Clopidogrel, Prasugrel, Ticagrelor** * **Inhibition of platelet activation by ADP** * Binds to and blocks the platelet Adenosive Diphosphate (ADP) receptor, causes decreased platelet activation & therefore thrombus formation USE: **Primary & Secondary relief for CVD, Anticoagulant prophylaxis**, ACS prevention * Can treat CVD without affecting BP SE: **GI irritation & bleeding** Interactions: **Antico****agulation drugs** *_The cloppy dog has 5 limbs (2+3) GPIIb and GPIIIa_*

Answer 4

* Comarin- Warfarin * Direct thrombin inhibitors- Dabigatran * Direct FXa inhibitors- Apixaban, Edoxaban, Rivarozaban * Heparins- Deltaparin, Tinzaparin, Enoxaparin (LMWH), Unfractionated heparin

Answer 5

Warfarin MOA: **Inhibition of vitamin K epoxide reductase** * Targets *extrinsic pathway* which inhibits vitamin K dependent synth of dependent clotting factors 10, 9, 7 and 2 (*1972*) (PT) * By inhbiting vitamin K carboxylation of the factors it decreases thrombin production USE: **Venous thromboembolism (DVT or PE) target INR 2.5, if recurrent 3.5** **Atrial fibrillation- Prophylaxis of stroke from AF target 2.5** **Mechanical heart valves - mitral valves generally require higher INR than aortic valves** SE: **Abnormal bleeding, teratogenic (can be used in breastfeeding), skin necrosis + purple toes.** Interactions: **NSAIDS, Diuretics,** (many others) NSAIDS potentiate warfarin by inhibiting platelets and displace warfarin from albumin P450 enzyme inhibitors - amioadrone and ciprofloxacin, increase warfarin action

Answer 6

Dabigatran MOA: **Competitive, reversible inhibitor of thrombin** * Direct inhibition of thrombin - thrombi cannot convert fibrinogen into fibrin and formation of secondary plug is inhibited Use: **Prophylaxis of VTE post-surgery** SE: - Interactions: -

Answer 7

**Apixaban, Edoxaban, Rivaroxaban** MOA: **Inhibition FXa in coagulation cascade** Use: **Prophylaxis of stroke from AF; DVT** SE: **Abnormal bleeding** Interactions: **-**

Answer 8

**Deltaparin, Tinzaparin, Enoxaparin (LMWH), Unfractionated Heparin** MOA**: Reversibly bind antithrombin III which inactivates thrombin and FXa.** * Unfractionated = Inactivated FXa & Thrombin * LMWH = Inactivated FXa Use: **Prophylaxis of VTE & PE** SE: **Abnormal bleeding** Interactions:-

Answer 9

* **Altepase** * **Streptokinase** * **Urokinase** MOA: **Activates plasminogen to plasmin for proteolytic breakdown of thrombus fibrin** (digests fibrin and fibrinogen to restore blood flow). Use: **MI, Ischaemic stroke** SEs: **N/A** * Arrhythmias, bleeding. Can only use streptokinase once as an immune response is generated againset the bacteria (streptococci) and memory B cells produce anti-streptokinase ABs. Interactions: -

Answer 10

* **Atorvastatin** * **Simvastatin** * **Rosuvastatin** MOA: **Inhibition of mavelonate pathway required for cholestrol synthesis (inhibits the rate limiting step in cholesterol synthesis).** * HMGCR enzyme is essential & rate-limiting in cholesterol synthetic pathway * HMGCR Inhibitors reduce circulating cholesterol levels, Promote uptake of excess cholesterol from bloodstream into liver Use: **Hypercholesterolaemia, Risk of CVD & Stroke** * CVD prevention WITHOUT affect BP SE: **Myopathy - myalgia, myositis, rhabdomyolysis and rise in creatinine kinase. Increased risk if older, female, low BMI and DBM.** **Liver impairment - check LFTs at baseline, 3 months and 12 months** Contraindications: Macrolide antibiotics use (erythromycin and clarithromycin) are an important interaction they increase the risk of rhabdomyolysis. Statins should be stopped until patients have completed the course. Interactions: **Verapamil, Macrolides** **\*Statins should be taken at night as this is when the majority of cholesterol synthesis takes place.** **\*\*** Treatment with statins should be discontinued if serum transaminase concentrations rise to and persist at 3 times the upper limit of the reference range.

Answer 11

* **Salbutamol (short acting)** * **Terbutaline (short acting)** * **Salmeterol (long acting)** * **Formoterol (long acting)** MOA: **Dilates bronchial smooth muscle** * Cellular Target: Bronchiolar Smooth Muscle * Molecular Target: Stimulation B₂ adrenergic receptors * B₂ agonists bind to *B₂-adrenergic receptors --\>* activation associated G protein --\> increases action adenylate cyclase. *AC* increases *cAMP levels/ action* in cytoplasm, activting protein kinase A (PKA). *PKA* **:** * Drives Ca²⁺ --\> Storage vesicles * Inactivates MLCK by reducing phosphyrlation --\> * This ^ plus less Ca²⁺ in Cytoplasm --\> reducation in smooth muscle contraction resulting in relaxation of smooth muscle in the airway. Use: **Asthma. Reversible airway obstruction** SEs: **Tremor, tachycardia,** cardiac arrythmia Interactions: **Diuretics**

Answer 12

* **Ipratropium (short acting)** * **Tiotropium (long acting)** MOA: **Blocks muscarining receptors --\> bronchiol dilation** * Cellular Targets: Bronchiolar smooth muscle cells. * Blocks *M3* muscarinic ACh receptors. * Actives G protein --\> Decreases action of *PLC:* reduces ca release from IC stores * Reducing Ca²⁺ release into the cytoplasm, reducing smooth muscle contraction causing bronchodilation. Use: **Acute asthma, Bronchospasms in COPD** SEs: **Dry mouth, constipation**, urinary retention Interactions:-

Answer 13

* **Theophylline** * **Aminophylline** MOA: **Bronchodilator, increases cAMP in smooth muscles** * Cellular targets: bronchiolar smooth muscle cells. * Mollecular targets: Blockage PDE * Binds to **B₂ adrenergic receptor**. Activation associated G protein. Increases action Adenylate cyclase- covnverts ATP --\> cAMP in Cytoplasms. This is normally inactivated by phosphodiesterase (PDE). * *Durgs block PDE sustains cAMP* levels activating PKA * Drives Ca²⁺ into storgae vesicles * Inactives MLCK by reducing phosphorylation * Less Ca²⁺in cytoplasm and reduced phosphorylation MLCK--\> Smooth muscle relaxtion--\> bronchodilation. Use: **Acute asthma, Reversible airways obstruction** SE: **Headache, Nausea** Interactions: **Antidepressants, Salbutamol**

Answer 14

* **Beclomethasone** * **Fluticasone** * **Prednisolone** * **Hydrocortisone** MOA: **Reduction of inflammation & mucus production** * Cellular target: Lung immune cells- Macrophages, T-lymps and eosinophils. * Molecular target: Intracellular GR * Activates the glucocorticoid receptor (GR) which interacts with selected nuclear DNA sequences and influences the expression of g=key genes: * Repression of pro-inflammatory mediators (TH2 cytokines) * Expression of anti-inflammatory products (B2 adrenoceptors) Use: **Asthma, Allergic rhinitis** SEs: **Cough** * MANY - Moon face, weight gain, osteoporosis, hyperglycaemia Interactions: **Aspirin**

Answer 15

* **Montelukast** * **Zafirlukast** MOA: **Blockade of leukotriene receptors** * Cellular targer: *Eosinophils & Bronchiolar Smooth Muscle* * Molecular target: Blocks *CysLT₁ leukotriene receptors.* * This reduces the inflammatory response in early and late phases of asthma * Additive effect when used with other drugs (eg: inhale glucocorticoids) * No evidence of effect on remodelling Use: **Asthma, Allergic rhinitis** SEs: **Abdo pain,** headache Interactions: **Phenobarbital**

Answer 16

Name: **Dornase Alfa** Use: **CF** MOA: **Synthetic DNAse 1- breakdown of extracellular DNA to reduce sputum viscosity**

Answer 17

MOA: **Increases dopamine synthesis & dopaminergic function** **Levodopa (DA precursor)** * Levodopa converts to dopamine as dopamine does not cross BBB - restores activity in the nigrostriatal pathway. **Pramipexole (synthetic agonist)** **Ropinirole (synthetic agonist)** **Rotigotine (synthetic agonist)** * DA Receptor agonist * Synthetic dopamine agonists stimulate D2 receptors on striatal neurons improving dopaminergic transmission. Use: **PD** * Synthetics used in younger patients SEs: **Confusion, Agitiation** * Anorexia, drowsiness, hypomania, hypotension, sudden onset sleep, 'on-off effects'**,** Arrythmia, Tachycardia * Synthetic more likely to have psych SE Interactions: **MOAI**

Answer 18

* **Carbidopa** * **Benserazide** ****MOA: **Stops breakdown of levadopa in periphery by inhibiting dopa-decarboxylase** * preventing GI and peripheral metabolism of levodopa meaning more is available to the CNS Uses: **PD** * Used with levodopa for Parkinsonism SE: **Confusion, Agitation** Interactions: -

Answer 19

* **Rasagiline** * **Selegiline** MOA: **Inhibits MAOI_B** **breakdown of dopamine** in the CNS Use: **PD** * Adjunct with levodopa/carbidopa for Parkonsonism SE: - Interactions: -

Answer 20

* **Entacapone** * Tolcapone MOA: **Blockade of dopamine precursor breakdown by inhibition of COMT** * Inhibits COMT **in the periphery** (outside CNS), reducing dopamine breakdown and allowing for more in the CNS Use: **PD** SE: **N&V** Interactions:-

Answer 21

* **Orphenadrine** * **Procyclidine** * **Trihexphenidyl** MOA: **Muscarinic cholinergic receptor antagonist** * in Parkinsons a decrease in dopamine lease to an increase in Ach concentration. Anticholinergics (antimuscarinics) readdress this balance). Use: **PD** (especially iatrogenic)**, Muscle rigidity, SE of anti-psychotics** * Iatrogenic PD (Orphenadrine) * Dystonia (Trihexphendyl & Procyclidine) SEs: **Dry mouth, Constipation** * may reduce absorption of levodopa Interactions:-

Answer 22

* **Tetrabenazine** MOA: I**nhibits VMAT₂** within basal ganglia, **preventing uptake of DA into vesicles** * Depletes serotonin, noradrenaline and dopamine. Dopamine is req for fine motor movement, so inhibition is helpful for kyperkinesis. Uses: **Huntington's** * Athetosis, Ballismus, Chorea SEs: - * Causes depression by decreasing 5HT and NA levels Interactions: -

Answer 23

* **Sertraline** * **Citalopram** * **Fluoxetine** MOA: **Inhibits 5HT reuptake pump in synaptic cleft-** increases 5HT levels. Use: **Depression/ GAD** SEs: **Insomnia, Nausea** * Sickness (nausea) sleep disorders- insomnia, sexual dysfunction, serotonin syndrome, slow onset. (5S's) * Seratonin syndrome = Overactiation ANS * Hyperthermia * CV Problems * Aggresion * Tremor * Rigidity Interactions: **Lithium, NSAIDS**

Answer 24

* **Moclobemide** MOA: **Inhibits MAO A** (in CNS) --\> **decreases breakdown of Na &5HT** * Reversible inhibitor of monoamine oxidase A (RIMA) Use: **Depression** SEs: **Tachycardia** * Cheese reaction: Postural hypotension, restlessness, convulsions, sleep disorders, * Cheese Reaction- increase tyramine which increases NA --\> Hypertensive crisis- vasoconstriction * "**S**ee **P**eople's **C**heese **R**eaction" *Interactions:* -

Answer 25

* **Amitriptyline** * **Nortriptyline** * **Dosulepin** MOA: **Na & 5HT reuptake inhibitor in synaptic cleft**. **a₁ adrenoreceptor antagonist, H1 receptor antagonist, M1 receptor antagonist** Use: **Depression, Neuropathic pain** SEs: **Anticholinergic syndrome** * Sedation (H1 blocker) * Dry mouth, constipation (M1 muscarinic blocker) * cardiac dysfunction (a1 adrenoreceptor blocker) Interactions: -

Answer 26

Overall Use: **Depression** Interactions & SE: - **Reboxetine** * **NRI** **Bupropion** * **Inhibits NA and dopamine reuptake** **Buspirone** * **Partial 5HT1a agonist** reduce activity to increase transmitter levels in the synaptic cleft **Agomelatine** * Melatonon agonist, increases slow wave sleep patterns. **Venlafaxine** * **?NRI** * SNRI - Inhibits reuptake of 5HT & Na **Mirtazapine** * **a2-adrenergic antagonist** * SE: Postural hypotension, Sleep disorder, Bronchoconstriction, Decreased HR Ruboxetine- Depression Venlafaxine- GAD/ PSTD/ Depression Busprione- GAD/ OCD/ Depression Mirtazapine- Depression Bupropion: Depression following smothin cessation

Answer 27

* **Chlorpromazine** * **Haloperidol** MOA: **Selective dopamine receptor blockade/ antagonists** * Also affect H1, M1 and a1 Use: **Schizophrenia** SEs: **Blurred vision, Tremor, EPS, Hypotension** * Tardive Dyskinesia (disabling involuntary movements) * Tongue Twisiting, Choreiform movements * Extrapyramidal symptoms * **Slowed movement** * **Tremor** * **Akasthisia,** * **Sedation** * Neuroleptic malignant syndrome: * Altered consciousness, Hyperthermia, Tachycardia, Incontinence * M1 receptor: Dry mouth, Constipation, Blurred vision * H1 receptor: Weight gain, Sedation * D2 Receptor: Slow movement, Rigidity, Prolactin elevation * Alpha1 Receptor: Hypotension, Drowsiness Interactions: -

Answer 28

MOA overall: **Selective D2 dopamine & 5HT receptor blockade** Use: **Schizophrenia** * **Amisulpride** ****5HT7 and Dopamine antagonist * **Risperidone** 5HT2A and Dopamine antagonist * **Clozapine** 5HT2A and domapine antagonist * **Olanzapine** Selective D2 and 5HT antagonist * **Quetiapine** Selective D2 and 5HT antagonist SE: **Hypotension, EPS** (- less likely: Akathisia, Tremor, Slowed movement, Sedation) * Neuroleptic Malignant Syndrome: Hyperthermia, Tachycardia, Altered Conciousness, Incotinence * D2 Anatagonist: Rigidity, Slow speech, Stiffness, Tremor * 5HT antagonist: Consiptation, Somnolence, Weight gain, Dizziness Interactions: -

Answer 29

* **Lithium carbonate** MOA**: Unclear but possible neuronal calicum channel blockade** Uses: **B****ipolar disorder** * Depression- resitant, recurrent unipolar as an adjunct to anti-depressants SE: **Tremor, hypothyroidism** Interactions: **NSAIDs, ACEi**

Answer 30

* **Donepezil** * **Galantamine** * **Rivastigmine** MOA: **Inhibitor of acetylcholinesterase (reversible)** Use: **mild- moderate AD** SE: **N&V** Interactions: -

Answer 31

* **Memantine** MOA: **VD blocker of NMDA receptors** (NMDA NAM) * Interferes with glutamate mediated cell death as prevents Calcium getting into cell Use: **Moderate to severe AD** SE: **Constipation & Hypertension** Interactions: -

Answer 32

*For both types:* Use: **Epilepsy** SE: **Nausea, Blurred vision** Interactions: **Macrolide abx** * **Sodium Valporate** * **Lamotrigine** * **Carbemazepine** MOA: **Block sodium channels** in the inactivated state Use: **Epilepsy** * All types of seizures except absence seizures SEs: Cognitive impairment, visual impairment, peripheral neuropathy, skin problems * **Ethosuximide - Ca2+ blocker** ****MOA: **Caclium channel blocker** * Targets low threshold voltage dependent T-type calcium channels Use: Absence seizures - first line

Answer 33

* **Midazolam -** GABA PAM (Y subunit) * **Lorazepam -** GABA PAM (Y subunit) * **Diazepam -** GABA PAM (Y subunit) * **Zolpidem** (BDZ like) MOA: **GABA PAM Y subunit**- opens Cl- channels --\> Cl- influx --\> Hyperpolarisation. **Enhanced effects of GABA** * GABA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present. Use: **Epilepsy, Acute seizures** SE: **Drowsiness, Dependence** Interactions: **Sedatives**

Answer 34

* **Flumazenil** MOA: **Antagonises GABA signalling** Use: **Reversal of BDZ signalling** SE:- Interactions:-

Answer 35

**Zopiclone** MOA: **Enhances GABA binding to GABA-A receptors** Use: **Insomnia** SE:- Interactions:-

Answer 36

* **Phenobarbitone-** GABA PAM (B subunit) * **Pentobarbitone-** GABA PAM (B subunit) * **Primidone-** GABA PAM (B subunit) MOA: **GABA PAM Beta subunit. Enhanced effects of GABA** * GABA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present. Use: **Epilespy, Acute seizures** * Status Epileptics * Primidone Essential Tremor SE: **Drowsiness, Fainting** Interactions: **Sedatives, Anticoagulants**

Answer 37

* **Paracetamol** Use: **Mild-moderate pain & fever** MOA: **Unclear- possible COX inhibitor in CNS** * No PG --\> * No prostanoid receptor activation --\> * Reduced activation VDNC SE: **Constipation** Interaction: **Warfarin** *In OD - conjugation (phase II metab.) pathway is saturated, phase I metab yields toxic metabolite NAPBQI which in high levels is toxic to hepatocytes --\> liver failure.*

Answer 38

* **Aspirin** * **Ibuprofen** * **Diclofenac** * **Naproxen** *Use:* **Mild- moderate pain, Inflammation** MOA: **Non selective COX inhibitors. Blockade prostaglandins synthesis** so less inflammation * Non selective COX inhibiton --\> No PG --\> No prostanoid receptor activation --\> Reduced activation VDNC SEs: * **GI side effects**- gastric ulcers and medication overuse headaches * **HTN** * **Not for under 16's** * Reye's Syndrome: Following viral infection asprin can cause RS (Fatty deposits in liver and brain) * NSAID intoxication: Salicylism (high dose of acute or chronic NSAID ingestion. Classic symptom = Tinnitus) *Interactions:* **Diuretics, ACEi**

Answer 39

* **Celecoxib** * **Etoricoxib** * Use:* **Inflammation,** Nociceptive **pain** * MOA:* **Selective COX 2 Inhibitor** --\> No PG --\> No prostanoid receptor activation --\> Reduced activation Voltage Gated Na+Channel. **Localised Pg blockade** * SE:* **Indigestion,** Thombosis Interactions: **ACEi & SSRI**

Answer 40

* **Codeine** * **Dihydrocodeine** * Use:* **Mild to moderate pain** * MOA:* **Opioid Receptor Agonist** --\> Decrease opening VDCC--\> Decrease Ca release from intracellular stores --\> Decrease exocytosis of transmitter vesicle and Increasing K outflow (post-synaptic) * SEs:* **Constipation, Nausea** * Resp depression, decreased GI motility, tolerance and dependance * Interactions:* **Sedatives** (Mimic endogenous opioids acting on opioid receptors to modulate pain at all CNS levels. Hyperpolarises the neuron so it is less likely to fire when a stimulus comes through)

Answer 41

* **Morphine** * **Diamorphine** * **Pethadine** * **Fentanyl** * MOA:* **Opioid Receptor Agonist** --\> Decrease opening VDCC--\> Decrease Ca release from intracellular stores --\> Decrease exocytosis of transmitter vesicle and Increasing K outflow (post-synaptic) * Uses*: Nociceptive **pain- severe** * SEs:* **Nausea,** **Constipation** * Resp depression, decr GI motility, tolerance and dependance, Vomiting, Mood alterations * Interaction:* **Sedatives**

Answer 42

* **Buprenorphrine** * **Pentazocine** * MOA:* **Opiod receptor modulation** * Opioid receptor partial agonist @ **Mu & Kappa Opioid Receptor** and Antagonist at delta * Use:* **Moderate-severe pain** * Maintenance therapy * SE:* **Constipation, nausea** * Interaction:* **Sedatives**

Answer 43

* **Naloxone (short lasting)** * **Naltrexone (longer lasting)** MOA: **Opioid receptor antagonist** * Compete for the same binding site as opioids, particularly the u receptor so reducing the effect of opioids Uses: **Opioid OD, Respiratory depresesion** * 2/ Prevent relapse of opiod/ alcohol abuse * SE:* **Nausea & Tachycardia** Interactions: -

Answer 44

* **Methadone** * **Buprenorphine** *MOA:* **Narcotic opioid replacement** (M) * Mu receptor, longer lasting. **Opioid r****eceptor agonist/modulator** (B) * Partial Mu and Kappa R agonist and antagonist at delta * Use:* **Maintenance therapy for opiod addiction.** * B for moderate to severe pain * SE:* **Constipation** * nausea (B) * Interactions:* * **Sedatives**

Answer 45

* **TCAs** * **(****Amitriptyline****- NRI, 5HTRI, H1 anatgonist, A1 antagonist, M1 antagonist)** * **Gabapentin** (AED) * MOA: **VDCC antagonist** * increases GABA transmission/ synthesis * **Pregabalin** (AED) * MOA: **VDCC antagonist** * ****increase GABA transport SE of all: **Dizziness, fatigue** Interactions of all: **Antidepressants** 4 types: Phantom limb, trigeminal neuralgia, post-stroke pain, post-herpetic pain (persistent pain after shingles). Y1 also included * **Carbamazepine** (AED) * MOA: Sodium channel blocker in inactivated state * ****SE: Teratogenic

Answer 46

Name: **NO & oxygen mixture** (Gas & air) Use: **Analgesia during childbirth** MOA: **Unclear** SE: **Decreased vitamin B12 synthesis** Interactions: -

Answer 47

*Inhaled:* * **Isoflurane** * **Sevoflurane** ****MOA: **Unclear, possible enhancement of GABA function** SE: **Hypotension** * Respiratory depression, Irritation of respiratory tract, Bronchospasm, Laryngospasm Interactions:- * IV:* * **Propofol** ****MOA: **Unclear, possible enhancement of GABA function** SE: **Hypotension** Interactions: - * **Ketamine** MOA: **NMDA (glutamate receptor antagonist)** * Blocks Ca & Na channels SE: **Hypotension** * Hallucinations, Raised HR and BP Interactions: - Y1: * Midazolam- GABA PAM y subunit * Can be used with no LOC IV Notes: * Decrease cardiac contracility * Respiratory depression * Decreased CNS function * Reduced sympathetic activity Ketamine/ Midazolam --\> Less CV/ Resp effects

Answer 48

* **Lidocaine** * **Bupivacaine** * **Levobupivacaine** MOA: **Voltage gated sodium channel blockade.** * Blocks voltage-gated Na⁺channels --\> Enter through cell membrane unionioned. Ionised IC space & block inside of Na channel * Not useful in inflamed tissue due to the acidic pH of 'inflammatory soup' reducinng effectiveness Uses: **Local anaesthetic** * Levobupivicane- Epidural Anaesthesia SE: **Rash** Interactions: -

Answer 49

Use for all: **Tracheal intubation & mechanical ventilation during surgery** SE: **Hypotension, Skin flushing** Interactions: - * Depolarising* : * **Suxamethonium (depolarising)** MOA: **Initial depolarisation & desensitisation of AChR** * Non-competitive, agonist * Bind AchR --\> Prologned depolarisation (receptor closes & repolarises w/ agonist still bound) --\> prevents further depolarisation * Fast onset, short duration *Non-depolarising* - (competitive, antagonist): * **Atracurium besilate (non-depolarising)** * **Vecuronium (non-depolarising)** MOA: **Competitive antagonist at AChR** * Bind AChR prevent depolarisation post synaptically. Pre synaptically reduced Ca entry --\> Less NT from pre-synaptic vesicle * Do not cross BBB * Slow onset, long duration \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_ _Y1:_ **Neostigmine** MOA: Peripheral inhibitor of acetylcholinesterase (depolarising) Use: Also used in MG AChEi: Increase Ach in junctional cleft, paralysis by overload- all AchR @ max SE: (PNS increase) Bradycardia, Increased secretions & Peristalsis

Answer 50

Use for all: **Immediate reversal of NMB to reduce post-op pulmonary complications** SE: - Interaction: - * For Non- depolarising:* * **Sugammadex** MOA: **Oligosaccharide that forms a complex with NMB, encapsulating and inativating it then removing them from NMJ** * ONLY for VECURONIUM * For ?Non-depolarising:* * **Neostigmine** MOA: **Peripheral inhibtor of acetylcholinesterase**- increasing Ach levels so neurone can fire again Use: + **MG** SE: Bradycardia

Answer 51

Use for all: **Maintain sedation & relaxed muscle tone** ***BDZ and BDZ like*** * **Temazepam**, **Zolpidem** Diazepam, Lorazepam, Midazolam * MOA: **GABA PAM Y subunit**. Open Cl^- channels --\> Hyperpolarisation. **Enhanced effects of GABA** * SE: **Drowsiness, Dependence** * Interactions: **Sedatives** ***Alpha-2 agonist*** * **Dexmedetomidine** * MOA: **Alpha-2 agonist inhbits sympathetic activity** * ****Inhibits NA release & terminates pain signals * SE: **Bradycardia** * Interactions:- ***Opioids*** * **Alfentanil, Fentanil, Remifentanil** * MOA: **Opioid receptor agonist** (Mu receptor) * Decreased opening VDCC --\> Decreased release Ca2+ from IC stores --\> Decreased exocytosis of transmitter vesicles. Increasing K outflow post-synaptically * SE: **Constipation, Nausea** * ****Respiratory depression, Miosis, Conscious depression, Constipation, Addiction/ tolerence * Interactactions: **Sedatives** * **Zolpidem (Z drug) -** GABA PAM (mechanistically identical to BDZ) * USE: Anxiety- short term crisis

Answer 52

Overall MOA: **Bactericidal - cell lysis by blocking cell wall synthesis** General uses: **Resp infections, Pneumonia, H.Pylori** Adverse Effects: **Rash, Hypersensitivity** Interactions: **Warfarin, Methotrexate** * ***Flucoxacillin*** * **SSTI** (use for **Staph** initially) * **Bone & Joint infections**- Empirical for ^ * **Penicillinase- Resistant** * ***Benzylpenicillin*** (NOT ON Y2) * **SSTI** (use for **strep**) * **Bone & Joint infections**- Empirical for ^ * ***Amoxicillin*** * **LRTI- CAP** * **Enhanced uptake by bacteria** * ***Co-amoxiclav*** * **Mixed infections** (eg: chronic chest), **UTI**, **Chronic bronchitis** * **Beca Lactamase Inhibitor** * ***Penicillin*** (not on Y2) * **Tonsillitis** **** * ***Piperacillin-Tazobactam*** * **HAP** **** * **Phenoxymethylpenicillin**

Answer 53

* **Meropenem** MOA: **Bacteriocidal - cell lysis by blocking cell wall synthesis** Use: **Meningitis, Hospital acquired septicaemia** * Infections in ITU & Complex, multi drug resistant infections SE: **Abdominal pain, Pruritis** Interactions: -

Answer 54

* **Ceftriaxone** MOA: **Bacteriocidal - cell lysis by blocking cell wall synthesis** Uses: **Meningitis**, **Gram negative infections** * Abdominal sepsis, Ortho infection SE: **GI disturbance, Colitis** * CDAD Interactions:- **Warfarin** NOtes: Later generations (like this one) Kill more natural flora & less effective against gram +ve infections. 10% of those with penicillin allergy are allergic to this

Answer 55

**Trimethoprim** MOA: **Inhibition of dihydrofolate reductase** * Nuclotide synthesis (folic acid) prevention Indications: **UTI** (primary care) Adverse Effects: **Rash, GI disturbance** Interactions: **Methotraxate**

Answer 56

* **Ciprofloxacin** MOA: **Inhibition of DNA gyrase** * Inhibition of bacterial DNA strucutre & function Use: **RTI** * UTI (secondary setting) * Gram -ve infections SE: **Nausea, Convulsions** * CDAD Interactions: **Iron salts, NSAIDS**

Answer 57

* **Erythromycin** * **Azithromycin** ****MOA: **Inhibition of bacterial protein** **synthesis** * Inhibit translation of mRNA. Inhibit bacterial protein/ RNA synthesis * Bacteriostatic Uses: **Pneumonia** * URTI, LRTI, SSTI, Atypical LRTI * SSTI in place of penicillin * Atypical LRTI ie: Legionella, Mycoplasma * Chlamydia in pregnancy SE: **Gi disturbance, Headache** Interactions: **Digoxin, Theophylline, Statins** * Affects drugs metabolised by CYP by inhibition thus increasing amount (warfarin, statins) * Caution in drugs that affect QT interval

Answer 58

* **Doxycycline** * **Tetracycline** MOA: **Bacteriostatic: Inhibition of bacterial protein synthesis** * Inhibit translation of mRNA. Inhibition of RNA & bacterial protein synthesis Use: **CAP** * Atypical bacteria lacking cell wall. Eg: Chlamydia, Mycoplasma Rickettsia infections, Typhus * +ve & -ve Bacteria SE: **Photosensitivity** * *GI Upset- Reflux Oesophagitis, Diarrhoea* * *Discolouration of tooth enammel in children* Interactions: - Notes: Do not give in pregnancy, breast feeding or U12

Answer 59

**Gentamicin** MOA: **Inhibition of bacterial protein synthesis- bacteriostatic** * Inhibits translation of mRNA. Inhibition of RNA & bacterial protein synthesis Use: **Opthalmic infections** SE:- Interactions:-

Answer 60

**Nitrofurantoin** MOA: **Bacterial DNA inteference** * Bacterial DNA structure and function inhibition Uses: **UTI** in primary healthcare setting Adverse reactions: **Peripheral neuropathy** Interactions: -

Answer 61

**Vancomycin** MOA: **Inhibition of cell wall synthesis in gram positive bacteria** * Cell wall inhibition Use: **C. Difficile** SE: **Neutropenia, Renal impairment** Interactions: -

Answer 62

* **Metronidazole** MOA: **Inhibition of bacterial DNA synthesis** * Bacteria DNA strucutre & function USE: **Anaerobic bacterial infections: leg ulcers, pressure sores** SE:- Interactions:-

Answer 63

**Rifampicin** & **Isoniazid** for 6 months **Ethambutol** & **Pyrazinamide** for 2 months MOA: * I, E: **Inhibition of mycobacterial cell wall synthesis** * R: **Inhibition of mycobacterial RNA synthesis** Adverse Reaction: **Hepatotoxicity** Interactions: -

Answer 64

Name: **Interferon alpha** MOA: **Activation of antiviral intracellular & immune response** Use: **HBV & HCV** Adverse reaction: **Flu-like symptoms, loss of appetite, lethargy, depression** Interactions:-

Answer 65

**Aciclovir & Ganciclovir** MOA: **Virus replication blockade** * --\> Aciclovir triphosphate. Competitively inhibits viral DNA polymerase incorporates into & terminates growing viral DNA chain & inactivates viral DNA polymerase Use: **HSV** SE: **Nausea & diarrhoea** Interactions: -

Answer 66

**Oseltamvir** MOA: **Prevention of viral budding & infectivity** * Clearves N viron to release from cell thus virion starts to die Indication: **Influenza virus infection** * LRTI acute bronchitis Adverse reaction: **Nausea & vomiting** Interactions:-

Answer 67

Name: **Ribavirin** MOA: **Disrupts viral RNA synthesis** Use: **HCV, RSV** Adverse reaction: - Interactions:-

Answer 68

Name: **Tenofovir** MOA: **Blockade of viral reverse transcriptase function for viral genetic replication** Use: **HIV,** Adverse reaction: **Rash, Stevens-Johnson syndrome** Interactions:-

Answer 69

Name: **Efavirenz** MOA: **Blockade of viral reverse transcriptase function for viral genetic replication** Use: **HIV** Adverse reaction: **Rash, Stevens-Johnson syndrome** Interactions:-

Answer 70

Name: **Lopinavir** MOA: **Blockade viral protease required for virus particle assembly** Use: **HIV** Adverse reaction: **GI Bleeding** Interactions:-

Answer 71

Name: **Dolutegravir** MOA: **Disrupts integration of HIV genome into host chromosome** Use: **HIV** Adverse reaction: **-** Interactions:-

Answer 72

Name: **Enfuvirtide** MOA: **Blockade of virus fusion to target cell membrane** Use: **HIV** Adverse reaction: **Pacnreatitis** Interactions:-

Answer 73

Name: **Maraviroc** MOA: **Blockade of HIV binding to co-factor for cell entry** Use: **HIV** Adverse reaction: **Nausea & diarrhoea** Interactions:-

Answer 74

Name: **Fluconazole** Use: **Candidia infection** MOA: **Disruption of fungal membrane function** SE: **Nausea & abdo pain** Interactions: -

Answer 75

Name: **Insulin** Use: **DMT1&2** MOA: **Stimulation of glucose uptake by cells** SE: **Hypoglycaemia** Interactions: **Digoxin & Beta blockers**

Answer 76

Name: **Metformin** Use: **T2DM - 1st line** MOA: **Increase insulin sensitivity- decreases hepatic gluconeogenesis, lipolysis, beta oxidation** SE: (Does NOT cause hypos or weight gain) * **GI --\> N&V, diarrheoa abdominal pain (20%) cannot tolerate it.** * Lactic acidosis in liver disease/ renal F Interactions: **Diuretics, digoxin** Started slowly and titrated up, 500 mg OD then titrated to twice daily to reduce the GI side effects. Maximum dose per day is 2g. Contraindication - * CKD with eGFR \< 30 --\> due to increased risk of lactic acidosis. * Recent MI / Sepsis / AKI /Dehydration / alcohol abuse

Answer 77

Name: **Gliclazide (**Glibenclamide, glimepiride) Use: **T2DM, 2nd line if metoformin not tolerated.** MOA: **Stimulates pancreatic insulin secretion** * Closes K+ channels (by glucose independent mechanism). Depolarisation results in Ca++ --\> exocytosis of insulin SE: * **Hypoglycaemia** * **weight gain** * **increased risk CV when used as monotherapy** * rarer --\> hyponatraemia, bone marrow suppression, hepatotoxicity and peripheral neuropathy Interactions: **Warfarin, NSAIDS** contraindications: avoid in pregnancy/ breastfeeding/ severe renal and hepatic impairment

Answer 78

Name: **Pioglitazone** Use: **T2DM** MOA: **Increases insulin sensitivity in muscle & adipose tissue** * Increases Beta cell preservation SE: (Do not cause hypos) * **Weight gain** * **Fluid retention - contraindicated in HF** * **Heart failure** * **anaemia** * **extended use can increase risk of bladder CA** * **increased risk of fractures**

Answer 79

Name: **Exenatide** (Dulaglutide, ***liraglutide)***"Tides" Use: **T2DM** MOA: **Incretin analogue- improves glucose control by increasing insulin secretion and inhibit glucagon secretion** Administered as a subcutaneous injection 2x / day or once weekly in modifiable release form. SE: * **GI tract upset** * **Asthenia/ weakness** * **weight loss and dizziness** * cardiac & cancer effects Contraindications: pancreatitis, renal impairment, severe liver impairment or GI disease.

Answer 80

Name: **Sitagliptin (Alogliptin, linagliptin (only one safe in renal impairment).** Use: **T2DM** MOA: DPP4 inhibitor therefore **Reduces inactivation of incretins** SE: * **Headache** * GI tract upset * pancreatitis, hepatitis, derangement of LFTs.

Answer 81

Dapagliflozin, canagliflozin, empagliflozin MOA: Inhibit SGLT2 therefore promotes loss of glucose in the urine Some evidence it reduces risk of CV disease Notable SEs: * Glycosuria therefore increased rate of UTI/ urosepsis (increased risk of fourniers gangrene) * genital inflammation * weight loss * DKA - rare * lower limb amputation with canagliflozin

Answer 82

Name: **Orlistat** Use: **Obesity especially in DMT2** MOA: **Inhibition of GI uptake of dietary fat** SE: **Oily stools, faecal urgency** Interactions: NA

Answer 83

* **Levothyroxine (Synthetic T₄)** * **Liothyonine (Synthetic T₃)** Use: **Hypothyroidism** MOA: **Synthetic hormone-** Activation of Thyroid Hormone Receptor * Mimics thyroid hormone by binding to incracellular alpha & beta thryoid receptors SE: **Diarrhoea, Vomiting** Interactions: **Oral anticoagulation**

Answer 84

Name: **Methotreaxte** MOA: **Inhibition of dihydrofolate reductase & DNA synthesis for lymphocyte proliferation** Use: **RA** SE: **Nausea,** **Hair loss** * Increased infection risk * Teratogenic; GI: Mouth Ulcers, Nausea, Diarrhoea * Hair loss Interactions: **Warfarin, Corticosteroids**

Answer 85

Name: **Azathioprine** MOA: **Unclear- possible inhibition of DNA synthesis & lymphocyte proliferation** * Purine antagonist Use: **RA & Crohn’s** SE: **Alopecia** * + (increased infeciton risk, teratogenic, mouth ulcers, nausea, diarrhoea) Interactions: N/a

Answer 86

Name: **Adalimumab, Etanercept, Infliximab** MOA: **TNF alpha blocker** Use: **RA** SE: **Infections** Interactions: NA

Answer 87

* **Sulphasalazine****** * **Mesalazine** MOA: **Mechanism unclear - possible COX inhibition. Possible free radical scavenging. T cell supression** Use: **RA, Crohn's** SE: **Nausea** Interactions: **Digoxin & Warfarin**

Answer 88

* **Desogestrel** & **Ethinyl- estradiol** Uses: **Hormonal Contraception, PCOS** * Dysmenorrhea, Menorrhagia MOA: **Mimics ovulation- reduces FSH** * (Low oestrogen has negative effect on AP inhibiting LH. Progesterone has negative effect on AP- inhibits LH & FSH) * MOA Molecular: Act on Oestrogen & Progesterone Receptors = INTRACEULLAR TRANSCRIPTION FACTORs- ER⍺and ERβ (Oestrogen) and PR-A, PR-B(Progesterone) * Steroid hormones = Hydrophobic molecules therefore diffuse across cell membrane to IC receptors * Hormone binding drives Receptor Activation viadissociation from HSP90 * Active Receptor Dimersform --\> Cell Nucleus & Influence Gene expression SE: **Weight gain, Depression, DVT** * Breakthrough bleeding, Nausea, Depression, Increased CV Risk (Oestrogen): IHD, Riased BP, THromboembolism, Stroke, Slight Breast Cancer risk w/ long term use Interactions:-

Answer 89

* **Desogestrel** * **Levonorgestrel** (emergency) MOA: **Mimics ovulation. Reduces LH & FSH. Endometrial changes** * Suppresses ovulation (negative feedback AP for LH and FSH) * Endometrium: Inhibits endometrial growth & makes mucus thicker preventing sperm/egg interaction *Cellular MOA:* * Intracellular Transcription Fractors: PR-A, PR-B * Steroid hormones = Hydrophobic molecules therefore diffuse across cell membrane to IC receptors * Hormone binding drives Receptor Activation via dissociation from HSP90 * Active Receptor Dimers form --\> Cell Nucleus & Influence Gene expression * Uses:* **Hormonal Contracpetion** * Dysmenorrhagia, Menorrhagia, Emergency contraception * SEs:* **Depression** * Slight increased risk of thrombotic events (stroke, DVT) and breast cancer. Breakthrough bleeding, Nausea, Vomiting Interactions: -

Answer 90

* **Etonogestrel** (long acting progesterone) MOA: **Mimics ovulation: reduces LH & FSH** * Moderate/high dose progesterone causing HPO ihibition suppresses ovulation. Also has mucus/endometrial effects. SEs: **Weight gain, Depression** * nausea, breakthrough bleeding Interactions:-

Answer 91

* **Estradiol** * **Norethisterone** * **Medroxyprogesterone** MOA: **Restore decreased hormone level & function** * Molecules cross membrane and bind to Intraceullar receeptors (INTRACEULLAR TRANSCRIPTION FACTORS)- ERalpha & ERbeta or PR-A & PR B. Binding drives Receptor Acitvation via dissociation from HSP90. Active Receptor Dimer forms --\> Cell nucleus & inflences gene expression. Uses: **Menopause** * Treats symptoms of menopause- hot flushes, vaginal dryness, sweats, loss of libido and reduces risk of osteoporosis. * Combination w/ Progestin avoid cystic endometrial hyperplasia SEs: **Weight gain, Depression** * Thromboembolism, Stroke. Breakthrough Bleeding, BReast tenderness, Increased breast cancer risk, Increased dementia risk \>65yrs Interactions:-

Answer 92

* **Dinoprostone** (Prostaglandin E2 aka PGE2) MOA: **Stimulates cervical ripening** Use: **Delay in labour** SE: - Interactions:-

Answer 93

* **Oxytocin** MOA: **Stimulate uterine contractions** Use: **Delay in labour** * delivery of the placenta in 3rd stage of labour SE: **Nausea, Arrythmia** Interactions:-

Answer 94

**Mifepristone with Misoprostol** ## Footnote MOA: **Steroidal antiprogesterone in combination with synthetic PG** Use: Termination in pregnancy SE: GI cramps, Uterine contractions, Vaginal bleeding Interactions: -

Answer 95

**TXA** ## Footnote MOA: Inhibits fibrin clot breakdown by plasmin Use: Menorrhagia SE: Nausea Interactions: -

Answer 96

**Mefanamic acid** ## Footnote MOA: **Inhibition of PG synthesis** Use: **Dysmenorrhoea** SE: **GI bleeding** Interactions:-

Answer 97

**Calcitonin** MOA: **Inhibits mobilisation of calcium from bones** * Decreases Ca2⁺ and PO₄ reabsorption in the kidneys, inhibits bone reabsorption by preventing osteoclast action (↓ serum Ca2⁺ and PO₄) Indications: **Osteoporosis, Hypercalcaemia** SE: **Abdominal pain** Interactions: **Antacids**

Answer 98

Alendronate, Pamidronate MOA: **Inhibits osteoclast function & bone resorption** * Slow rate of bone remodelling: * Absorbed onto hydroxyapatite crystals * When osteoclasts begin to resorb that bone with bisphosphonate, bisphosphonate released & impairs osteoclast ability to form ruffled border to adhere to bony surface & produce protons necessary for bone resorption * Can also decrease osteoclast progenitor development & recruitment * Can promote osteoclast apoptosis Indications: **Osteoporosis, Hypercalcaemia** SE: - Interactions: -

Answer 99

**IV calcium gluconate, Vitamin D, Parathyroid hormone** MOA: **Restoration of calicum levels & metabolism** * IV calcium gluconate * ****Replaces lost calcium in the body * Vitamin D * vit D in activ form Calcitriol prevents Ca2+ and PO4 excretion from the kidney and increases reabsorption in the intestines Indications: **Hypocalcaemia, Bone loss** SE: **-** Interactions:-

Answer 100

* **Vitamin D (colecalciferol, calcitriol, 1,25-dihydroxyvitamin D)** MOA: **Restoration vitamin D levels** * Replaces vit D - active form Calcitriol prevents Ca2+ and PO4 excretion from the kidney and increases reabsorption in the intestines. Indications: **Vitamin D deficiency** SE: - Interactions: -

Answer 101

Raloxifene MOA: **Stimulation of oestrogen function in bone** * Inhibition of release of Ca from bone & Inhibition of Osteoclast activity * Agonist: stimulate bone formation * Antagonist to receptors in breast & uterine tissue Indications: Prevention of bone fractures SE: Hot flushes Interactions: Warfarin

Answer 102

Denosumab MOA: **Inhibition of osteoclast function & bone resorption** * Monoclonal antibody (similar to OPG which binds to RANKL- from OB to prevent RANKL attaching to RANK on OC) * Inhibits osteoclast formation, function & survival Indications: Osteoporosis SE: Hypocalcaemia Interactions: -

Answer 103

Name: **Prednisolone, Hydrocortisone, Dexamethasone** MOA: **Intracellular transcription factor interactions, gene expressions (inhibition). Inhibit production of IL-1 to 8 & TNF-alpha** Use: **Suppression of inflammatory diseases (RA, crohn’s, UC)** SE: **Weight gain, Muscle atrophy** Interactions: **PO antidiabetics**

Answer 104

Name: **Cyclosporin, Tacrolimus** MOA: **Inhibition of T cell signalling- inhibits function or maturation** Use: **Solid organ transplant to prevent rejection & Eczema** SE: **HTN** Interactions: **Aspirin**

Answer 105

Name: Chlorphenamine MOA: H1 histamine receptor blockade Use: Hay fever, Urticaria SE: Dry mouth, Sedation Interactions: TCA

Answer 106

Name: **Cyclophosphamide** MOA: **Cross linkage and damage to DNA** Use: **Broad spectrum of malignancies** SE: **Hair loss, bone marrow suppression & nausea** Interactions: NA

Answer 107

Name: **Paclitaxel, Docetaxel** MOA: **Inhibition of microtubule assembly in mitotic spindle** Use: **Broad spectrum of malignancies** SE: **Hair loss, bone marrow suppression & nausea** Interactions: -

Answer 108

Name: **Vincristine, Vinblastine** MOA: **Inhibition of microtubule assembly in mitotic spindle** Use: **broad spectrum of malignancies** SE: **Hair loss, bone marrow suppression & nausea** Interactions: -

Answer 109

Name: M**ethotraxate** MOA: **Inhibition of dihydrofolate reducatase and DNA synthesis** Use: **Broad spectrum of malignancies and RA** SE: **Increased infection risk, Teratogenic, GI: Mouth Ulcers, Nausea, Diarrhoea; Hair loss** Interactions: -

Answer 110

Name: **Fluorouracil, Cytarabine** MOA: **Inhibition of RNA and DNA synthesis** Use: **Broad spectrum of malignancies** SE: **Hair loss, bone marrow suppression & nausea** Interactions:-

Answer 111

Name: **Mercaptopurine, Thioguanine** MOA: **Inhibition of RNA & DNA synthesis** Use: **Broad spectrum of malignancies** SE: **Hair loss, bone marrow suppression & nausea** Interactions: -

Answer 112

Name: **Doxorubicin** MOA: **DNA intercalation. Inhibition of RNA & DNA synthesis** Use: **Broad spectrum of malignancies** SE: **Hair loss, bone marrow suppression & nausea** Interactions: -

Answer 113

Name: **Trastuzumab, Rituximab, Nivolumab** MOA: * **Target cells overexpressing Human epidermal growth factor- 2 (HER2) for tumour reduction & destruction** * **Bind & Block proinflammatory function CD20 on B cells** * **Stimulation of anti-tumor responses via blocking PD-1** Use: * **Early breast cancer** * **Follicular lymphoma, Non-hodgkin’s lymphoma,** Rejection, RA, SLE * **Melanoma** SE: * **Fever and chills** * **Fever and chills** * **-** Interactions: -

Answer 114

Name: **Lenolidamide** MOA: **Stimulation of T cell response** Use: **Myeloma** SE: **Foetal risk** Interactions: -

Answer 115

Name: **Tamoxifen** MOA: **Inhibition of ER function & cell proliferation in breast.** Partial Agonist of Oestrogen Receptors. Inhibition of release of Ca from bone & Inhibition of Osteoclast activity * Agonist: Stimulate bone formation * Antagonist to receptors in: Breast & Uterine tissue Use: **Breast cancer** & osteoporosis SE: * Thromboembolism, Stroke * Breakthrough bleeding, Breast Tenderness * Increased Breast Cancer Risk * Increased Dementia Risk \>65yrs Interactions: -

Answer 116

Name: **Goserelin** MOA: **Synthetic analogue of LHRH. Activates LHRH receptor function --\> sustained testosterone reduction** Use: **prostate cancer** SE: - Interactions: -

Answer 117

Name: **Ferrous sulphate** Use: **Iron deficient anaemia** MOA: **Iron Provision** SE: **Constipation** Interactions: **Antacids**

Answer 118

Name: **Folic Acid (B9)** Use: **Folate deficient anaemia** MOA: **Supports nucleic acid synthesis** SE: - Interactions:-

Answer 119

Name: Vitamin B12 parenteral Use: Pernicious anaemia MOA: Enzyme co-factors SE:- Interactions: -

Answer 120

Class I: Sodium channel blockers Class II: Beta blockers Class III: Potassium channel blockers Class Iv: Calcium channel blockers (phenylalkylamine & benzothiazepine subclasses)

Answer 121

MOA: **Voltage sensitive sodium channels blockage- *prolonged QT interval, increase QRS duration*** SE: **Oedema** Interactions:- **Class 1a:** * *Name*: **Disopyramide, Quinidine** * *MOA extra:* Delays depolarisiation * *Use:* **Ventricular & Supraventricular arrhythmias** **Class 1b)** * *Name*: **Lidocaine** * *MOA extra:* Blocks sodium channel in actively depolaring cells. AP shortened * *Use:* **CPR used IV** **Class 1c)** * *Name*: **Flecainide, Propafenone** * *MOA extra:* Slight reduction in phase 0, no change in AP duration * *Use:* **Paroxysmal AF & ventricular ectopic beats-**"pill in pocket"

Answer 122

**Atenolol** (beta-1), **Bisoprolol** (beta-1), **Metoprolol** MOA: **Beta- adrenergic receptor blockade-**reducation in adrenergic effects on rate & intropy Use: **Proplylaxis of paroxysmal atiral tachy or AF** SE: **Hypotension** Interactions: **NSAIDs, Digoxin** *From CVS section* MOA: **Negative inotropic/ chrontropic agent** * Competitive inhibitors of adrenaline and noradrenaline at B-adrenoceptor sites. Inhibit sympathetic stimulation of heart muscle. * Heart Specific: B1 antagonists are selective for the cardiomyocytes: Negative inotropes & chronotropes. Reduce workload on the heart relieving oxygen demand. * Molecular Mechanism in the heart: Blocked Beta-adrenergic receptors. Less ATP --\> cAMP by Adenylyl Cyclase. Less Protein Kinase (PK) A activity. Less release of Ca from SR- Less free Ca inside cell. Less contraction Uses: **HTN, Stable angina** SEs: **Bradycardia, Bronchospasm**, Dizziness, constipation

Answer 123

**Amiodarone, Dronedarone, Sotalol** (has so beta blocker activity) ## Footnote MOA: **Potassium channel blockade & caclium channel blocker properties- *prolonged QT interval*** (delay repolarisation therefore prolongs the action potential.) Use: **Supraventricular, nodal & ventricular tacharrythmias, AF** SE: **N&V** Interactions: - amiodarone with warfarin

Answer 124

**Verapamil, Diltiazem** MOA: **Calcium channel blockade- *reduction of AP & cardiac output*** * Reduces amplitude of phase 2- reduced intracellular calcium thus -ve inotropic on myocytes Use: **SVT (especially paroxysmal)** SE: **Hypotension (verapamil), Constipation (diltiazaem)** Interactions:-

Answer 125

**Digoxin** MOA: **Reduces conductivity of AVN** Use: **Arrythmias- AF, CHF** SE: **Fatigue & Nausea** Interaction:-

Answer 126

**Adenosine** MOA: **Activates adenosine receptors --\> hyperpolarization & slows conduction through AVN** * Binds A1 receptors in pacemaker tissues. Inhibts AC, reduces cAMP, K+ efflux increases --\> hyperpolarised cells Use: **SVT** SE: **Nausea** Interactions: * CONTRAINDICATED- **obstructive airway disease**

Answer 127

**Atropine** MOA: **Blockade of vagal muscarining Ach receptors** * Blocks type M2 Ach receptors on cardiomyocytes * Inhibits PS effects- cholinergic vagus transmission exerting negative chronotropy * Atropine accelerate repolarisation in cardiac muscle Use: **Emergency bradycardia** SE: **Urinary rentention** Interactions:-

Answer 128

**Magnsium sulphate (IV)** MOA: **Unclear. Aleration of Na+, K+, Ca2+ ion balance via channels & transporters** * Stabalise AP Use: **Emergency arrythmias, IV emergency in asthma** SE: **Electrolyte irregularities** Interactions:-

Answer 129

**Cyclizine** MOA: **Histamine H1 receptor blockade** Use: **Nausea, Vomiting** SE: **Dry mouth, Sedation** Interactions: **Sedatives**

Answer 130

**Domperidone** MOA: **Dopamine D2 receptor blockade in chemoreceptor trigger zone** Use: **Nausea & Vomiting** SE: **Cardiac disease**

Answer 131

* **Oxybutinin** MOA: **Competitively** antagonizes the **muscarinic 2/3 acetylcholine receptor** leading to **smooth muscle relaxation** and reduction of bladder detrusor activity Use: **OAB** SE: **Dry Mouth, Tachycardia** (preceded by transient bradycardia) * Blurred vision, Constipation, , Urinary Retention

Answer 132

Tamulosin ## Footnote MOA: Smooth muscle relxant aciting on bladder neck Indication: BPH, urinary retention SE: Dizziness Interactions: Hypotensive drugs

Answer 133

Mirabegron ## Footnote MOA: Stimulates beta-3 adrenergic receptors --\> detrusor smooth muscle relaxation Indication: OAB SE: Bladder pain Interactions: -

Answer 134

**Finasteride** MOA: **Inhibits synthesis of dihydrotestosterone** Use: **BPH** SE: **Impotence** Interactions: -

Answer 135

N-Acetylcysteine MOA: Restoring & maintaining hepatic intracellular glutathione required for paracetamol detoxifcation Indication: Paracetamol OD SE: Oral inflammation

Answer 136

Chlordiazepoxide MOA: Potentiation of GABA-A receptors Indication: Severe alcohol misuse SE: Dizzy, Drowsy

Answer 137

Clomethiazole MOA: GABA mimetic, GABA-A receptor agonist Use: Severe alcohol misuse SE: Nasal congestion

Answer 138

Acamprosate MOA: GABA mimetic, GABA-A receptor agonist. Possible NDMA receptor antagonist Use: Severe alcohol misuse SE: Diarrhoea & Nausea

Answer 139

Fondaparinux Fondaparinus is a syntehtic pentasaccharide than inhibits activated factor X. Indications : NSTEMI and UA.

Answer 140

Ivabradine MOA: Inhibition of cardiac I(f) current in SA node. Antianginal drug that works by reduced the heart rate acting on the "funny current" in the SA node reducing pacemaker activity. Uses: Angina with normal sinus rhythm & heart failure Use in heart failure - only if in sinus rhythm \> 75 bpm and LVEF under 35% Adverse effects: * visual effects - luminous phenomena * headache * bradycardia and heart block

Answer 141

Amiodarone - class 3 antiarrhythmic agent used in the treatment of atrial, nodal and ventricular tachycardias. Main MOA by blocking K+ channels therefore inhibiting repolarisation and prolonging the action potential. Limitations: * long half life * ideally given into central vein as causes thrombophlebitis * proarrythmic effects by prolonging QT interval * decreases the metabolism of warfarin as P45O inhibitor Long term effects: * Thyroid dysfunction - hypo and hyper * corneal deposits * pulmonary fibrosis / pneumonitis * liver fibrosis / hepatitis * peripheral neuropathy and myopathy * photosensitivity & slate grey skin * thrombophlebitis at injection sites * bradycardia and long QT interval Monitoring needed: - TFT, LFT, U & E and CXR prior to tx - TFT, LFT needed every 6 months

Phase III drug list Flashcards

Welcome to my drugs list deck. They should contain the MOA + usage & side effects that we need to know for every drug on the list. Some cards have ways to remember the drugs/picture prompts... also if there are any mistakes/any could be refined or made better please let me know and ill edit!