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Pharmacology 2002 - Coggle Diagram

- - - - should not be used with beta blockers
      - preferred for the treatment of supraventricular tachycardia
  - - - efficacious orally active vasodilator
      - topical minoxidil (rogaine) used as a stimulant for hair growth for correction of baldness
      - should not be combined with beta blocker and loop diuretics
    - - used in treating hypertensive emergencies + severe cardiac failure
      - activation of guanylyl cyclase
- - - - H1 - Gq coupled to Phospholipase C (PLC)
        
        smooth muscle, endothelium, CNS
        
        bronchoconstriction, vasodilation, pain and itching, allergic rhinitis, motion sickness
      - H2 - Gs coupled to adenylyl cyclase (AC)
        
        gastric parietal cell, vascular smooth muscle cell, basophils
      - H3
        
        CNS cells, some peripheral NS
      - H4
        
        highly expressed in bone marrow and white blood cells
  - - - chlorpheniramine
        
        antipsychotic
      - promethazine
        
        prophylactic for motion sickness
      - diphenhydramine (benadryl)
      - cyclizine (antivert) + meclizine
        
        prevent motion sickness
    - - fexofenadine (allegra)
        
        weak sedation, reccommended for workers
      - desloratadine
      - levocetirizine (xyzal)
      - terfenadine (seldane) and astemizole (hismanal) were removed from the market - prolonged QT interval
    - - cimetidine, famotidine
        
        used in treatment of peptic ulcers
      - must be prescribed with B12 under normal conditions since HCl secretion is decreased
- - - - prevent inactivation of monoamines within a neuron
      - selegiline : used in treatment of depression and Parkinson's disease
    - - effective treatment for depression in patients in whom SSRIs are ineffective
      - sibutramine (weight loss)
    - - fluoxetine (prozac)
  - - - all are GPCRs except 5-HT3 (ligand-gated Na+ channel)
  - - - ketanserin = 5-HT2A/2C antagonist (treatment of hypertension)
      - clozapine = atypical antipsychotic, 5-HT2A/2C antagonist
      - agomelatine = new antidepressant with agonist action at the melatonin receptor and antagonism at 5-HT2C
    - - ondansetron
      - palonosetron
      - treatment of chemotherapy-induced nausea and vomiting
- - - - primary prevention of arterial disease
      - secondary prevention of myocardial infarction and stroke
      - lowers serum cholesterol in patients with homozygous familiar hypercholesterolemia
    - - myopathy, rhabdomyolysis,
        muscle weakness -> myoglobinuria
      - GIT disturbance, rash, angioedema
  - - - inhibits intestinal absorption of phytosterols and cholesterol
  - - - cholesterol-lowering in statin intolerant patients
- - - - side effects: diarrhea, nausea, vomiting
        headache, dizziness, tinnitus
      - cardiac effects: prolongs action potential duration
    - - only drug for ventricular fibrillation
      - preferred for treatment for ventricular tachycardia
      - not used for atrial fibrillation
    - - weak beta blocker
      - sodium channel blocker
      - may cause constipation, metallic taste
  - - - peripheral vasodilation
      - slowing of heart rate
        
        symptomatic bradycardia and heart block may be expected
      - slow delayed rectifier potassium current blocked
      - may result in hypo/hyperthyroidism
      - prolongs action potential duration
      - sinus node depression
      - abnormal liver function tests and hepatitis may develop during treatment. The skin deposits result in a photodermatitis and a gray-blue skin discoloration in sun-exposed areas, eg, the malar regions
  - - - suppresses aferdepolarisations
      - should not be used with beta blockers
      - preferred Ca++ channel blocker for supraventricular tachycardia treatment
    - - not used for the treatment of ventricular tachycardia
  - - - only useful for supraventricular tachycardia
      - effect is too short
      - not cardiodepressive
- - - - alpha receptors
        
        A1 : a = first letter in the alphabet
        first thing when you see a tiger. you become pale
        VASOCONSTRICTION
        
        relaxes skeletal muscle*
        
        constricts urethral sphincter
        
        mydriasis
        
        SELECTIVE A1 AGONIST : phenylephrine
        
        nasal decongestant + ophthalmologic use
        
        vasopressor (when given IV)
        
        constricts veins, skin, blood vessels
        
        RISE IN BP + INCREASE IN PERIPHERAL VASCULAR RESISTANCE
        
        often evokes compensatory reflex bradycardia
        
        A2 : decrease smooth muscle constraction
        
        SELECTIVE A2 AGONIST (presynaptic) : clonidine
        
        pain killer
        
        antihypertensive
        
        Sympatholytics
        
        Alpha blockers
        
        Non-selective
        
        Irreversible: phenoxybenzamine
        
        used to treat hypertension due to pheochromocytoma
        
        Reversible
        
        phentolamine
        
        1 more item...
        
        tamsulosin
        
        1 more item...
        
        side effect : reflex tachycardia
        
        Selective
        
        Alpha 1 (prazosin, terazosin, doxazosin, alfuzosin)
        
        Side effects: tachycardia, postural hypotension (when they start the medication they should take it at night), nasal congestion, headache due to cranial vasodilation
        
        1 more item...
        
        Alpha 2 (yohimbine - was used as an aphrodisiac)
        (mirtazapine - research drug, antidepressant)
        
        other side effects: miosis, nasal stuffiness
      - beta receptors
        
        B1 : benim bir kalbim var
        
        increases heart rate
        
        increases force of contraction
        
        increase renin release (kidney)
        
        SELECTIVE B1 AGONIST : dobutamine (heart failure)
        
        B2 : benim iki akcigerim var (smooth muscle relaxation)
        
        relaxes bronchi
        
        decreases mucus production (reduced airway resistance)
        
        SELECTIVE B2 AGONIST : salbutamol
        
        drug of choice to treat acute asthmatic bonchoconstriction
        
        ritodrine, terbutaline : used in premature labor, may be hazardous to both mother and fetus
        
        both B1 & B2 agonist : isoprenaline (bradycardia)
        
        Beta blockers
        
        non-selective
        
        -ISA
        
        nadolol (longest half-life = 10-20h)
        
        propranolol (crosses blood-brain barrier)
        
        used in pathological tremor, social anxiety
        
        used in thyrotoxicosis (hyperthyroidism)
        
        timolol
        
        used in glaucoma
        
        +ISA
        
        pindolol
        
        B1 selective
        
        atenolol (5-8h, relatively longer half-life)
        
        bisoprolol (11-17h)
        
        esmolol (shortest half-life, 9 mins)
        
        present in IV preparations, used in emergency settings
        
        metoprolol
        
        acebutolol (partial agonist)
        
        With alpha-blocking activity
        
        carvedilol
        
        used in cardiac heart failure
        
        labetalol
        
        can be used on pregnant patients
        
        used in hypertensive emergencies
        
        decrease heart rate, force, automaticity, cardiac output, cardiac oxygen consumption + hypoglycemia
        
        antidote for overdose of beta blockers = glucagon
      - both alpha and beta agonsit : adrenaline, noradrenaline (direct acting)
        amphetamine (indirect acting)
        ephedrine (both)
        
        drug of choice for immediate treatment of anaphylactic shock (adrenaline/epinephrine)
      - D1 agonist : dopamine, fenoldopam (very useful in treatment of renal failure related with shock)
  - - - receptors : muscarinic & nicotinic
        
        M1 (most important organ = brain) : central nervous system
        
        cognitive functions (memory)
        
        M2 (2nd most important organ = heart)
        
        M3 : everywhere
      - cholinergics
        
        direct acting
        
        muscarinic (alkaloids, cholinester)
        
        nicotinic
        
        indirect acting (anticholinesterase)
        
        physostigmine (only one that crosses the central nervous system)
        
        IRREVERSIBLE : echothiophate
      - stimulation : miosis, accommodation to near vision
      - antagonism: mydriasis (dilation of pupil)
        accommodation to a far vision
      - anticholinergic drugs
        
        antimuscarinic
        
        M1 selective (pirenzepine)
        
        peptic ulcer, reduce gastric secretion and muscle spasm
        
        Nonselective (atropine)
        
        atropine overdose
        
        hot as a hare (increased temperature - hyperthermia
        decreased sweating)
        
        mad as a hatter (confusion, delirium)
        
        red as a beet (flushed face, tachycardia)
        
        dry as a bone (decreased secretions, thrist)
        
        blind as a bat (mydriasis & cycloplegia - paralysis of circular muscles of the eye = blurred vision, loss of accommodation)
        
        used for mushroom poisoning
        
        antinicotinic
        
        ganglion blockers (hexamethonium)
        
        neuromuscular blockers (tubocurarine)