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Pharmacology - Coggle Diagram

- - - - Pilocarpine (Alkaloid)
        
        Non-selective muscarinic alkaloid
      - Bethanechol (Choline ester)
        
        M3 muscarinic agonist
      - Used for glaucoma
    - - Physostigmine
        Neostigmine
        Rivastigmine
        Donepezil
        Tacrine
        
        Reversible anticholinesterase inhibitor - donates carboxyl group
        
        Donepezil/tacrine used in slowing down progression of Alzheimer's
    - - Ecothipate
        Dyflos
        Sarin
        Parathion
        Organophosphates
        
        Irreversible anticholinesterase inhibitor - donates phosphate group
  - - - Hexamethonium
        Trimetophan
        Alpha-bungarotoxin
        
        Anti-hypertensive
    - - Atropine
        Glycopyrrolate
        Hyoscine
        Scopolamine
        Tropicamide
        Procyclidine
        Trihexyphenidyl
        Ipratropium bromide
        Oxybutynin
        
        Tropicamide - dilate pupil in retina examination
        
        Hyoscine - prevent motion sickness
  - - - Adrenaline
        
        a and b receptors
    - - Phenylephrine
        
        a1 > a2 > b
      - Clonidine, Brimonidine (A2)
        
        a2 > a1 > b
    - - Isoprenaline (B1/2)
        
        b > a
        
        Side effect - reflex tachycardia
      - Dobutamine (B1)
        
        b1 > b2 > a
      - Salbutamol / Ventolin
        
        b2 > b1 > a
        
        Used for asthma, relax uterus and prevent contractions in premature labour
        
        Side effects - reflex tachycardia, tremor, diabetes
    - - Cocaine
        
        Blocks monoamine reuptake system -> increase NA/DA in synapse
      - Tyramine
        
        Competes with catecholamine for uptake 1
  - - - Propanolol
        
        b1 and b2 antagonist
      - Atenolol
        Metoprolol
        Bisoprolol
        Esmolol
        
        b1 antagonist
      - Aide effects - bronchoconstriction, bronchospasm
        b1 - cardiac failure
        b2 - hypoglycemia
    - - Phentolamine
        
        a1 - vasodilation, reduce BP
        a2 - increase NA release - enhance reflex tachycardia
      - Prazosin
        
        a1 antagonist
        
        Side effect - postural hypotension -> reflex tachycardia
    - - Labetalol
        Carvedilol
        
        a1 b1 dual antagonist
    - - Methyldopa
        
        lower effect on a1 receptor, greater effect on a2 receptor
        
        for pregnant women
  - - - Sinnamet
        Madopar
        
        More efficacious than dopamine agonist
        
        Side effects
        Nausea and vomiting (CTZ) - give domperidone
        Hallucination
        Dyskinesia
        Hypotension
        
        Effectiveness of L-DOPA declines over time due to loss of neurons eith disease progression
    - - Bromocriptine
        Ropinerol
        
        Side effect 1st gen - heart valve problem
        
        Side effect 2nd gen - addictive behaviour
        
        Acts on D2 receptors in striatal cells
        
        Lower incidence of dyskinesia
        Smoother more sustained therapeutic response
    - - Apomorphine
    - - Selegiline
        Rasagiline
        
        Rasagiline has anti apoptotic effect on bcl-2 gene - neuroprotective effect
    - - Tolcapone (CNS + PNS)
        Entcapone (PNS)
    - - Amantidine
        
        Increase dopamine release per nerve impulse
        Prevent dopamine reuptake
    - - Procyclidine
        Trihexyphenidyl
        
        Loss of dopamine in striatum -> increase in cholinergic neuronal activity -> tremor block M4 receptors -> remove D1 inhibition
  - - - Phenytoin
        
        Blocks voltage gated Na channel -> prevent depolarisation and reduce number of action potentials
        
        Used in status epilepticus
        
        CYP450 inducer
        
        Side effect - gingival hypertroph
      - Carbamazepine
        
        Blocks voltage gated Na channel -> prevent depolarisation and reduce number of action potentials
        
        First line in partial seizures
        
        Check HLA B*1502 to avoid SJS/TEN
        
        CYP450 inducer
    - - Used in generalized seizures - 1st line
      - CYP450 inhibitor
      - Side effects - severe hepatic toxicity, acute pancreatitis
        Teratogenic - neural tube defects (spina bifida)
- - - - Aspirin + warfarin
        
        increased risk of GI bleeding
      - Tolbutamide + insulin
        
        Increases risk of hypoglycemia (can be used carefully in DM)
      - ACEi + thiazide
        
        Hypotension (can be used carefully in hypertension)
    - - Diphenhydramine (antihistamine) + Ethanol
        
        Affects mental function
      - Paracetamol + tramadol (opioid)
        
        streong analgesic effect - beneficial
      - LABA + corticosteroid
        
        Bronchial dilation in asthma - used in inhalers
    - - Naloxone
        
        locks action of opioids - antidote in opioid overdose
      - Folic acid
        
        Reduces efficacy of methotrexate
      - Vitamin K
        
        Decreases action of warfarin
- - - - (-azines)
        (-penthixols)
        Haloperidol
        Pimozide
        Sulpiride
        
        Decreases dopamine activity in mesolimbic and striatal region
        
        Use for Huntington's Disease (lack of GABA in basal ganglia - excess dopamine in putamen causing hyperkinesive chorea and jerks)
        
        Side effect - extrapyrimidal effects
        
        Acute dystonia, tardive dysknesia, neuroleptic malignant syndrome, endocrine (increased prolactin and hypogonadism, gynecomastia)
  - - - Equally effective to typical antipsychotics
      - Clozapine used for resistant schizophrenia
      - Side effects
        
        Endocrine (blocking D2 receptors - increased serum prolactin and hypogonadism - lactation, gynecomastia, galactorrhea, amenorrhea - more commoon than typical antipsychotics)
        
        Alpha receptor - orthostatic hypotension
        
        5-HT receptor - weight gain"
        
        mACh receptor - dry mouth, constipation, blurred vision,redness - especially clozapine
        
        Glucose intolerance
        
        Extrapyrimidal symptoms and neuroleptic malignant syndrome - risperidone highest risk
        
        Clozapine - agranulocytosis
  - - - Fluoxetine
        Fluvoxamine
        Sertraline
        Citalopram
        Escitalopram
        Paroxetine
        
        1st line treatment for depression
        
        Inhibits CYP450
        
        Dangerous when used with MAO
        
        Side effects:
        Acute phase - nausea, GI symptoms, insomnia, headache
        Long term - sexual dysfunction
    - - Vanlafacxine
        Densvenlafaxine
        Duloxetine
        
        2nd line treatment for depression when SSRIs are ineffective
        
        Side effects - nausea, headache, sexual dysfunction, insomnia, hypertension
    - - Imipramine
        Amitriptyline (1st gen)
        Nortriptyline (2nd gen)
        Desipramine
        Trimipramine
        Protriptyline
        
        Rarely used due to extensive side effects and narrow therapeutic range
        
        serotonin = noradrenaline > dopamine
        
        Amitriptyline in MDD - can cause mania/hypomania
        
        1st gen inhibits CYP450
        2nd gen - toxicity equal to SSRI, safer than 1st gen/SNRI
        
        Side effects - antimuscarinic (mydriasis, bowel bladder decrease motility, reduced sweating, reduced secretion)
        Alpha block postural hypertension
        QTc prolonged - cardiac dysrhythmia (most common cause of overdose) - induce torsades
        Sodium bicarbonate therapy treats widened QRS and ventricular arrhythmia
        Sexual dysfunction, seizures
    - - Hydrazines (Isocarboxazid, Nialamide, Phenelzine)
        Iproniazid
        Meclobemide
        
        Prevent metabolism of monoamine - increase duration of receptor activation
        MAO-A - 5HT = NA > DA
        MAO-B - DA
        
        Cheese reaction - less breakdown of tyramine, displaces NA from vesicles, increase NA release - hypertensive crisis
        Hypotension
    - - Buproprion
        
        CNS activating effects
        
        Side effects - dose-dependent increased risk of seizures (avoid if seizure risk or bulimia nervosa or anorexia nervosa), hypertension
    - - Nefazodone
        Trazodone
        
        Side effects - priapism (trazodone) due to a1 blockade (avoid in sickle cell anaemia and multiple myeloma)
        Hepatotoxicity (nefazodone), orthostasis
    - - Mirtazapine
        
        Helps with loss of appetite and inability to sleep
        
        Side effects - weight gain, increase in cholesterol, sedation
  - - - Analgesic, antipyretic
      - Adult - max 4g/day
        Paeds - max 75mg/kg/day
      - Metabolised in liver - if acute liver failure - treat with IV N-acetyl cystein to remove reactive metabolite
    - - Celecoxib
        Parecoxib
        Etoricoxib
        
        lipophilic
        
        Celecoxib - sulfonamide - avoid for sulfa allergy
    - - Irreversible - Aspirin
        Reversible - Ibuprofen, indomethacin, naproxen
        
        Block COX - increase endocannabinoid -> analgesia
        Block COX - more 5-lipooxygenase metabolism - bronchoconstriction/spasm
        
        Effect of PGE2
        Stimulate PG receptor on nerve ending, sensitise nociceptors - pain
        Stimulate hypothalamic neuron - increase body temperature
        more Th17
        Th1 differentiation
        
        Adverse effects
  - - - Donezepil
        Rivastagmine
        Tacrine
        
        Rivastigmine - both acetylcholine and butylcholinesterase
        Increases amount of ACh in synapses between bucleus basalis of Meynert and hippocampus, amygdala, frontal cortex implicated in alzheimer's
    - - Memantine
        
        Decreases excitotoxic actions of excess glutamate from amyloid plaques and neurofibrillary tangles
  - - - Cannabis
        Marijuana
        Hashish
        Weed
        Dope
        Ganja
    - - Cocaine
        Crack
        Freebase
      - Tobacco
        Nicotine
- - - - Promethazine
        
        H1 > M > D2
        
        Motion sickness prophylaxis (even after it occurs)
        Use for hyperemesis gravidarum (step up to metoclopramide then ondansetron)
    - - Hyoscine
        Scopalamine
        
        M > D2 = H1
        
        Motion sickness prophylaxis (only before)
    - - Domperidone
        Metocloriamide
        Haloperidol
        Prochlorperazine
        
        D2 > H1 > M
        
        Acts on CTZ
        Prokinetic effects - increase stomach emptying, increases LES pressure, decreases smooth muscle motility, acceleratedmovement of food content
        
        Metoclopramide - crosses BBB
        Domperidone - does not cross BBB
        
        Side effect - extrapyrimidal effects - Parkinsonian like syndrome - rigidity, tremor, akathisia, tardicve dyskinesia
    - - Aprepitant
        Fosaprecipitant
    - - Ondansetron
        
        Prolongs QT interval and induces torsades
        
        Serotonin syndrome - rigidity, hyperthermia, confusion
        
        Acts of vagal efferent of GI tract and CTZ
  - - - Sodium bicarbonate
        
        Side effect - Constipation (Al, Ca), Diarrhoea (Mg)
    - - Omeprazole
        
        Irreversible inhibitor of H/K/ATPase
        
        H.pylori triple therapy
        GERD
        ZES
        
        Side Effect - C. difficle diarrhoea
        
        First line for treating NSAID caused ulcer
    - - Cimetidine
        Ranitidine
        Nizatidine
        Famotidine
        
        Competitive antagonist of H2 receptors on parietal cell, reducing effect of histamine by producing enterrochromaffin cells
        
        CYP450 inhibitor
        
        First line for PUD, Second line for GERD
    - - Venoprazan
        Revaprazan
        Tegoprazan
        
        Used for GERD
    - - Sucralfate
        
        Acquires strong negative charge in acid environment, forms gel like complex to coat ulcer
        
        Increases prostaglandin, mucus, bicarbonate secretion - reduced H. pylori
        
        May cause constipation
        Reduces absorption of other drugs
    - - Bismuth chelate
        
        Coats mucosa
        
        Part of triple therapy against resistant H. pylori
    - - Misoprostol
        
        Contraindicated in pregnant women
        
        Side effect - diarrhoea
    - - Clarithromycin
        Amoxicillin (or metronidazole)
        PPI
  - - - Mesalazine
        Olsalazine
        
        Mesalazine - active on its own, in small bowel and colon
        
        Olsalazine - requires activation by guy flora, only active in colon
        
        Maintain UC remission, treat active disease
        Maintain surgically-induced remission of CD
    - - Prednisolone
        Budesonide
        Fluticasone
        Hydrocortisone
        
        Drug of choice for inducing remission in CD
        
        Anti-inflammatory and immunosuppressive
    - - Azathioprine
        
        Activated in vivo to 6-mercaptopurine - interferes with purine synthesis to affect DNA synthesis
        
        Maintain remission of UC and CD
    - - Methotrexate
        
        Folate antagonist - reduce synthesis of thymidine and purines
        
        Not widely used due to significant side effects - avoid in pregnancy
    - - Cyclosporin
        
        Lowers T cell activity by calcineurin-phosphatase pathway, prevents mitochondrial permeability transition pore from opening
        
        Severe UC, prevent rejection of solid organ transplant
    - - Infliximab
        Adalimumab
        
        High increase in risk of infections for TB and Hep B
- - - - Tranexamic Acid (TXA)
        
        Inhibits activation of plasminogen to plasmin, binds to both plasminogen and plasmin
  - - - Clopidogrel
        Prasugrel
        Ticagrelor
        
        Clopidogrel is antiplatelet of choice
        
        ADP receptor (P2Y12) Inhibitor
      - Aspirin
        
        COX inhibitor - stops thromboxane A2 formation
        
        Side effect - gastric ulcer, bronchospasm in severe asthmatics
        
        Prolonged bleeding time - cease 5-7 days bfore invasive procedure
        
        Reye's syndrome - acute viral illness, acute encephalopathy, liver disease
      - Abiciximab
        
        Monoclonal IgG antibody against GpIIb/IIIa - prevents binding with vWF and fibrinogen
    - - Warfarin
        
        Inhibits vitamin K epoxide reductase
        Factor VII is first clotting factor to be reduced when starting warfarin
        
        Stop if INR >8
        Goal INR 2-3
      - Unfractionated Heparin
        
        Binds antithrombin III - irreversibly inactivates thrombin and factor Xa
        Reduce effects of Factor II, IX, X and XI
        
        Monitor via aPTT
        
        Acts on Factor II
      - Low molecular weight heparin (-parin)
        
        Monitor via anti-Xa
        
        Reduce effects of Factor II, IX, X and XI
        
        Acts on Factor X
      - Fondaparinux
        
        ATIII Activator
    - - Bivaluridin
        Dabigatran
        Rivaroxaban
        Apixaban
        
        To reverse dabigatran - activated charcoal (within 2 hours), haemofiltration (more than 2 hours)
        
        Cannot be taken with impaired renal function - prefer warfarin
        
        Interacts with clarithromycin
        
        Rivaroxaban, Apixaban - FXa Inhibitor
        Dabigatran - FIIa Inhibitor - direct thrombin inhibitor
        Bivalirudin - FIIa Inhibitor - direct thrombin inhibitor
    - - Streptokinase
        Alteplase
        
        Tissue plasminogen activator, cleaves plasminogen to produce active plasmin, decrades fibrin -> clot disolution
        
        Gold standard treatment for ischaemic stroke, only after clot is pre-formed