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MVST 1B (Fach) / MoDA (Lektion)

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• Paracetamol* Use: Analgesic for mild to moderate pain; antipyretic MoA: NSAID; selective COX-3 inhibitor SE: Liver damage in overdose (→ N-Acetyl-Cysteine) Dose: 0.5 - 1 mg PO every 4-6 hours; max 4g daily → co-codamol, co-dydramol; ibuprofen, diclofenac, aspirin
• Penicillamine Use: Immunosuppressant in rheumatoid arthritis, Wilson's disease SE: Membranous glomerulonephritis → nephrotic syundrome →pyridoxine, isoniazid, gold
• Phenothiazines Class of neuroleptics (e.g. → chlorpromazine) and antiemetics (e.g. → promethazine) Ca2+/CaM dependent PDE-I inhibitors, D2-receptor antagonists
• Promethazine Use: hayfever, anaphylaxis, nausea/vomiting, vertigo, motion sickness; allergy, urticari; sedation MoA: 1st generation antihistamine SE: drowsiness → chlorphenamine*, mepyramine; cetirizine/fexofenadine/loratidine; chlorpromazine
• Ranitidine Use: GORD, Peptic Ucler Disease, SSc MoA: H2-receptor blocker, ↓acid secretion from GPC's SE: Diarrhoea → cimetidine; omeprazole/lansoprazole, gaviscon
• Etoricoxib Use: Osteoarthritis, ankylosing spondylitis, reumatoid arthritis MoA: Selective COX-2 inhibitor SE: less GI; palpitations, fatigue, flu-like symptoms →Celecoxib
• Sulfasalazine Use: Active rheumatoid arthritis, inflammatory bowel (active Crohn's, UC active and in remission) MoA: Immune modulator, related to aspirin SE: Stephen-Johnson syndrome, pancreatitis, reversible oligospermia, pancytopaenia → methotrexate, infliximab, hydroxychloroquine; mesalazine
• Sumatriptan Use: Acute migraine, cluster headache MoA: Serotonin analogue → 5-HT1B/1D agonist; cerebral vasoconstrictor to treat migraine SE: tingling, heat, heaviness, flushing, dizziness, dyspnoea; contra-indicated in IHD, recent MI → NSAIDs, aspirin, paracetamol; ergotamine→ propranolol, topiramate, valproic acid
• Tacrolimus Use: Prophylaxis of rejection in solid organ (liver, heart, kidney) allografts; moderate-to-severe atopic ezcema MoA: Immunosuppressant; inhibits calcineurin, IL-2 secretion, T-cell proliferation ~ciclosporin; → azathioprine/mycophenolate, steroids; sirolimus, cyclophosphamide
• Terfenadine Use: Seasonal allergic rhinitis, chronic idiopathic urticaria MoA: prodrug → fexofenadine = non-sedating anti-histamine → loratidine, cetirizine
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• Triamcinolone Use: Joint injections in inflammation / pain, rheumatic disease MoA: Long-acting synthetic corticosteroid SE: initial flare-up; osteoporosis/-necrosis, diabetes, cataracts, weight gain, infection. →hydro-/fludrocortisone, prednisolone, beclamethasone, methylprednisolone
• Theophylline Use: Severe acute asthma MoA: non-selective PDE-inhibitor; mast cell stabiliser, competitive adenosine receptor antagonist SE: GI upset; palpitations, arhythmias, headache → aminophylline, magnesium sulphate
• Zafirlukast Use: Asthma (Step 4) MoA: LT-receptor antagonist ~ montelukast; → zileuton
• Zileuton Use: Asthma (step 4) MoA: 5-LOX inhibitor; inhibits leukotriene synthesis → SABA (sabutamol, terbutaline), ICS (beclamethasone, budosenide), LABA (salmeterol); zafirlukast/montelukast
• Desmoteplase Plaminogen activator from vampire bats Clinical trials for <9h after stroke, not yet licensed
• Zolpidem Use: Insomnia MoA: Positive GABA_A modulator at benzodiazepine binding site; not a benzodiazepine  SE: GI upset, CNS symptoms: agitation, memory disturbance, confusion, derpession, dependence ~ zopiclone, eszopiclone, zaleplon
• Buspirone 5-HT-1A-receptor agonist Anxiety
• Tiagabine Use: Anti-epileptic; adjunct for focal seizures ± 2ary generalization MoA: GABA reuptake inhibitor → sodium valproate, lamotrigine; carbamazepine; ethosuximide; levetiracetam
• Vigabatrin Use: Anti-epileptic for focal seizures ± 2ary generalization; last line MoA: GABA transaminase inhibitor → GABAA enhancer SE: Visual field defects, behavioural changes → tiagabine
• Sodium valproate Use: Epilepsy: Tonic-clonic, juvenile, etc (all forms), migraine prophylaxis MoA: Succinic semialdehyde dehydrogenase (SSADH) inhibitor (GABA metabolism);p Na+ channel blocker SE: Weight gain, alopecia; neural tube defects (→5mg folic acid), craniofacial abnormalities (valproate syndrome)  Usually sodium valproate = Epilim → carbamazepine, lamotrigine, phenytoin, levetiracetam, topimarate
• Diazepam Clinical use: anticonvulsant, anxiolytic, status epilepticus, insomnia, peri-operative MoA: Benzodiazepine GABAA receptor agonist SE: drowsiness, confusion amnesia, aggression ~ flunitrazepam, clonazepam, lorazepam, midazolam, oxazepam, chlordiazepoxide, etc.
• Flumazenil Use: iatrogenic benzodiazepine overdose; reversal of sedative effects MoA: GABAA receptor antagonist SE: nausea and vomiting Dose: 100-300mcg repeated IV injections, max 2g
• Phenytoin Use: acute symptomatic seizures, status epilepticus MoA: Na+ channel inhibitor, SE: fever, ataxia. coarse tremor, liver fibrosis, pancreatitis, arrythmias → lorazepam, diazepam, midazolam→ valproate, lamotrigine, carbamazepine, ethosuximide
• Ethosuximide Use: Absence seizures MoA: T-type Ca2+ channel blocker SE: GI disturbance ~trimethadione; → sodium valproate, lamotrigine, carbamazepine, levetiracetam, phenytoin
• Gabapentin Use: Epilepsy (focal ± 2ary generalization), peripheral neuropathic pain MoA: L-type Ca2+ channel blocker SE: GI-upset, dry mouth, weight gain, hypertension, ... →pregabalin
• Desipramine NA-selective TCA, Dibenzazepine → amitriptyline, nortriptyline, imipramine, clomipramine; venlafaxine
• Clomipramine Non-selective TCA; Dibenzazepine
• Nortriptyline Use: Depressive illness; neuropathic pain MoA: NA-selective TCA; Dibenzcycloheptenes SE: Antimuscarinic, restlessess, fatigue →amitriptyline, clomipramine, trimipramine, dosulepin
• Citalopram Use: Depressive illness, panic disorder MoA: 5-HT-selective TCA; SSRI SE: GI upset, anorexia, hypersesitivity rash → fluoxetine, sertraline
• Venlafaxine Use: Major depressive disorder; generalized anxiety disorder MoA: SNRI, 5-HT > NA SE: antimuscarinic ~duloxetine, reboxetine
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• Tranylcypromine Use: Depressive illness MoA: Irreversible MAO-A-inhibitor SE: postural hypotension, insomnia, dizziness   ~ phenelzine; moclobemide
• Moclobemide Use: Depressive illness, social anxiety disorder MoA: Reversible MAO-A inhibitor (RIMA), reduced "cheese effect" SE: sleep disturbances, dizziness, gastro-intestinal disorders, headache, restlessness, agitation; paraesthesia, dry mouth, visual disturbances, oedema, skin reactions, confusional states reported → SSRI's (fluoxetine, sertraline, citalopram); traylcypromine
• Atypical antidepressants Buproprion -- DAT, NET nACh-receptor antagonist Mertazapine -- monoamine receptor antagonist Nefazodone -- 5-HT-1, 5-HT-2, α1 antagonist Agomelatine -- melatonin-receptor antagonist Vortioxetine -- SSRI, 5-HT-1 agonist; fewer side effects Tianeptine -- SERT enhancer (!)
• Bromocriptine Use: prolactinoma MoA: ergot-derivative partial D2-receptor agonist SE: retroperitoneal fibrosis → cabergoline; ropinirole, pramipexol, apomorphine
• Haloperidol Use: Schizophrenia, behavioural problems in mentally retarded, nausea in palliative care MoA: D2>D1-reecptor antagonist; typical 1st generation neuroleptic SE: Extrapyramidal x4, hormonal x2, atimuscarinic; malignant euroleptic sydrome (→dantrolene) → chlorpromazine, fluphenazine; risperidone; clozapine, olanzapine, quetiapine
• Chlorpromazine Use: Schizophrenia, mania, agitation; nause in palliation MoA: Non-selective dopamine receptor antagonist; 1st generation typical neuroleptic SE: extrapyramidal x4, hormonal x2 antimuscarinic → haloperidol, fluphenazine; risperidone, quetiapine, olanzapine, clozapine
• Clozapine Use: Schizophrenia, psychotic side effects of Parkinson's medication MoA: Selective D2-like-receptor antagonist; 2nd generation neuroleptic SE: Weight gain, exrapyramidal (parkinsonism, dystonia, akathisia, tardive dyskinesia), hypotension agranulocytosis, myocarditis → Olanzapine, quetiapine; haloperidol, risperidone
• Tolcapone Use: Parkinson's + cocareldopa MoA: COMT-inhibitor that crosses the BBB SE: GI upset, hepatotoxic →co-carel/benel-dopa; ropinirole, pramipexol; rasigiline, selegiline; entacapone; procyclidine, benzatropine
• Rasagiline Use: Parkinson's disease MoA: MAO-B-inhibitor →selegiline
• Benzatropine Use: Drug-induced  Parkinsonism, excl. tardive dyskinesia; Parkinson's disease; dystonia MoA: mACh-recepor antagonist; inhibits antagonist neostriatal loop; treat Parkinsonian side-effects of neuroleptics (D2-antagonists) SE: dry mouth, constipation/urinary retention, blurred vision, confusion, etc. → procyclidine
• Levodopa Use: Parkinson's disease MoA: Dopamine precursor SE: on/off effects, dyskinesia; nausea, vomiting, dry mouth, postural hypotension, psychosis → carbidopa/benserazide, co-careldopa/co-beneldopa; ripinorole, selegiline, entacapone
• Risperidone Use:Psychosis, persistent aggression MoA: Atypical antipsychotic; action at D2, 5-HT, glutamate receptors SE: Weight/appetite gain, hypertension, exprapyramidal symptoms → clozapine, olanzapine, quetiapine; haloperidol, chlorpromazine, fluphenazine
• Donepezil Use: Mild to moderate dementia in Alzheimer's, "Aricept" MoA: AChE-inhibitor SE: GI upset, fatigue, aorexia, insomnia   ~ Tacrine, rivastigmine, galantamine; → amantadine
• Thioperamide H3-receptor antagonist; promote wakefulness and memory consolidation
• Xylometazoline Use: nasal congestion MoA: α-adrenoreceptor agonist → ephedrine
• Salmeterol Use: asthma, COPD MoA: long-lasting β2-receptor agonist → salbutamol/terbutaline
• Dabigatran Use: Anticoagulation MoA: direct thrombin inhibitor →bivalirudin,
• Misoprostol Use: Gastric ulceration (adjuvant of NSAIDs); abortion, induction of labour MoA: synthetic PGE2-analogue; protects gastric mucosa; stimulates uterine contractions SE: Diarrhoea →omprazole/lansoprazole; ranitdine/cimetidine; gaviscon→iloprost, lanasoprost
• Isoniazid Use: Tuberculosis, 1st lie w/ other drugs MoA; Mycolic acid synthesis inhibitor; SE: Peripheral neuropathy (→pyridoxine) → rifampicin, pyrazinamide, ethambutol; D-cycloserine, streptomycin
• Memantine Use: Moderate to severe dementia in Alzheimer's disease MoA: NMDA glutamate receptor antagonist; open channel blocker. SE: constipation; hypertension; dyspnoea; headache, dizziness, drowsiness → donepezil, revostigmine

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