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1

1.  Pharmacodynamics I (Molecular targets of drugs. Drug receptors. Receptor theory.)

Molecular targets of drugs:

A. Receptors:

  • IC receptors
    • Nuclear
    • Cytopalsmic
  • Transmembrane ligand-gated receptors
    • Tyrosine-kinase
    • Jak-STAT
  • Transmembrane ligand gated ion channel
  • G-protein coupled receptors
    • Class I: Rhodopsin-like
    • Class II: Secretinin-R-like
    • Class III: Metabotropic Glu-R-like

B. Enzymes:

  • Reversible inhibitors
  • Irreversible inhibitors

C. Transport proteins

D. Voltage-gated ion channels

  • Na+ channels
  • K+ channels
  • Ca2+ channels

E. Other

  • Nucleic acids
  • Microbial targets
  • Structure proteins

2

2. Pharmacodynamics II (relation between drug dose and clinical response, therapeutic index, tolerance, pharmacodynamic drug interactions)

A. Relationship between drug dose and clinical response:

  • Effects of drug concentration on receptor binding
    • Affinity
  • Graded dose-response:
    • Efficacy
    • Potency
  • Dose-response relationship
    • Dose-response curve
    • Quantal (cumulative) dose-response curve
      • Therapeutic index

B. Intrinsic activity:

  • Agonism
    • Full agonist
    • Partial agonist
      • Duality
      • Spare receptors
    • Inverse agonist
  • Antagonism
    • Competitive: increased EC50, unchanged Emax
    • Non-competitive
      • Irreversible: Increased EC50, decreased Emax
      • Reversible allosteric: unchanged EC50, decreased Emax

C. Selectivity:

  • Pharmacodynamic selectivity
  • Pharmacokinetic selectivity

D. Repeated administration:

  • Tolerance (decreased response)
  • Sensitization (increased response)

E. Pharmacodynamic drug interactions:

  • Synergism
  • Antagonism
  • Neutral

3

3. 3. Drug absorption, distribution and bioavailability. Membrane transport mechanisms.

A. Absorption:

  • Transport mechanisms:
    • Passive diffusion
      • Aqueous diffusion
      • Lipid diffusion
    • Carrier-mediated transport
      • Facilated diffusion
      • Active transport
        • Transporters
          • Influx
          • Efflux
    • Endocytosis, Exocytosis
  • Ionization
    • ​Effect of pH on drug absorption
  • Other factors influencing absorption
    • ​Blood flow
    • Total surface area
    • Contact time
    • Expression of P-glycoprotein

 

B. Routes of administration:

  • Enteral
    • Oral
    • Sublingual
  • Parenteral
    • ​IV
    • IM
      • Aqueous solution (fast absorption)
      • Depot preparation (slow absorption)
    • Subcutaneous
  • Others
    • ​Oral inhalation
    • Nasal inhalation
    • Intratheca//intraventricular
    • Topical
    • Transdermal
    • Rectal
    • Cutan
    • Eye drops

C. Bioavailability:

  • Definition
  • Determination of bioavailability
  • Factors influencing bioavailability
    • 1st pass effect
    • Solubility of drug
    • Chemical instability
    • Nature of the drug formation

D. Distribution:

  • Blood flow
  • Capillary permeability
  • Binding of drugs to plasma proteins and tissues
    • Plasma proteins
      • Albumin
      • Drug activity
      • Binding influences
    • Tissue proteins
  • Special barriers of distribution
    • Placenta
    • CNS
    • Fat
  • Volume distribution (Vd)
    • Apparent volume of distribution
    • Redistribution
    • Compartments based on perfusion
      • Central compartments
      • Peripheral compartments
      • Deep compartments
    • Effect of Vd on half-life

4

4. Drug biotransformation, linear and non-linear kinetics. Enzyme inhibition and induction. Clearance, half-life, loading and maintenance dose. Elimination. Pharmacokinetic drug interactions

A. Metabolism - Biotransformation:

  • Phase I
    • The P-450 system
      • Definition 
      • P-450-dependent oxidative reactions
      • P-450 independent oxidative reactions
      • P-450 inducers
      • P-450 inhibitors
      • Reaction with P-450
      • Reactions without P-450
  • Phase II
    • Conjugation reactions
      • Glucuronidation
      • Acetylation
      • Glutathione conjugation
      • Methyl conjugation
      • Sulfation
  • Pharmacogenetics:
    • Genetic polymorphism

B. Elimination:

  • Renal elimination
    • Glomerular filtration
    • Proximal tubular secretion
    • Distal tubular secretion
  • Biliary elimination
  • Lungs - exahalation
  • Skin

C. Kinetics:

  • Zero order elimination (non-linear)
  • 1st order elimination (linear)
  • Half-life
  • Clearance
  • Steady state
    • Plateau principle
    • Effect of loading dose

5

5. Cholinergic transmission and its presynaptic modification. Ganglion blocking agents.

A. Cholinergic neurotransmission

  • Acetylcholine:
    • Synthesis
    • Storage
    • Release of ACh
    • Binding to receptor
    • Degradation of ACh
    • Recycling of ACh
  • Main cholinergic transmissions
    • CNS
    • Autonomic ganglia (PSY and SY)
    • NMJ
    • PSY postganglionic nerve
    • Certain SY postganglionic nerves (sweat glands)
  • Cholinergic neuroeffector junction
    • Receptors
      • Nicotinic receptors
      • Muscarinic receptors
  • Presynaptic modification
    • ​Stimulation
      • 4-aminopyridine
      • alpha-latrotoxin
      • Increase calcium
      • Inhibition of presynaptic inhibitory receptors
      • Nerve sitmulation
    • Inhibition
      • Hemicholinum
      • Vesamicol
      • Botulinum toxin
      • AChE inhibitors
      • Recptor antagonists

B. Nocotinic receptor antagonists:

  • Ganglionic blockers
    • Competitive
      • Tertiary amines
        • Mecamylamin
        • Trimetaphan
      • Quaternary amines
        • Hexamethonium
        • Tetraethylammonium
    • Non-competitive
      • Nicotine
    • Inhibition

6

6. Adrenergic transmission and its presynaptic modification

A. Adrenergic neurotransmission:

  • Transmission
    • Synthesis
    • Storage
    • Release
    • Binding
    • Termination
    • Fates of recaptured NE
  • Adrenoceptors:
    • alpha, beta, D1
    • Desensitization of receptors
  • Structure-activity relationship

B. Presynaptic modification:

  • Stimulation
  • Inhibition

7

7. Cholinomimetics

A. Direct acting cholinomimetics:

  • Muscarinic (mainly)
    • Choline esters
      • ACh
      • Bethanechol
      • Carbachol
      • Methacholine
      • Synthetic drugs:
        • Cevimeline
        • Varenicline
    • Alkaloids
      • Pilocarpine
      • Lobeline
      • Arecoline
      • Nicotine
      • Muscarin

B. Indirect-acting cholinomimetics (AChE inhibitors):

  • Reversible
    • Edrophonium
    • Physostigmine
    • Rivastigmine
    • Neostigmine
    • Pyridostigmine
    • ambenomium
    • Demecarium
    • Donepezile
    • Tacrine
  • Irreversible
    • Organophosphates
  • Toxicity of AChE inhibitors

8

8. Muscarinic receptor blocking drugs

A. Atropine:

  • Peripheral effects
  • CNS effects

B. Parasympatholytics:

  • Clinical uses
  • Tertiary tropeins
    • Atropine
    • Scopolamine
    • Homatropine
    • Benztropine
  • Quaternary amines
    • Ipratropium
    • Methylalatropine
    • Tiotropium
  • Synthetic drugs with tertiary amine
    • Procyclidine
    • Biperiden
    • Tropicamide
    • Pirenzepine
    • Tolterodine
    • Oxybutynin
    • Solifenacine
    • Darifenacine
  • Synthetic drugs with quaternary amine
    • Propantheline

9

9. Catecholamines

A. Catecholamines:

  • Properties
    • High potency
    • Rapid inactivation
    • Poor CNS penetration
    • Administration
  • Drugs
    • Epinephrine
    • Norepinephrine
    • Isoproterenol
    • Dopamine
    • Dobutamine

B. Non-catecholamine direct-acting sympathomimetics:

  • Selective beta1 agonists
    • Ibopamine
    • Prenalterol
  • Selective beta2 agonists
    • ​Main actions and indications
      • Bronchodilators
        • LABA
          • Salmeterol, formoterol
        • SABA
          • Metaproterenol, salubtamol, terbutaline, fenoterol, pirbuterol
      • Relaxation of pregnant uterus
        • Ritodrine, terbutaline
    • Adverse effects
  • Selective beta3 agonists
    • Mirabegron
  • Peripheral D1 receptor agonists
    • Dopamine
    • Fenoldopam
    • Dopexamine
  • Non-selective alpha agonists
    • Oxymetazoline, xylometazoline
  • Mixed adrenergic agonists (sympathomimetics)
    • Ephedrine
    • Pseudoephedrine
    • Phenylpropanolamine

10

10. Indirect sympathomimetics. Selective alpha1-agonists. Selective alpha2-agonists and drugs acting on the imidazoline receptors

A. Indirect sympathomimetics:

  • Releasers:
    • Amphetamine
    • Tyorsine
    • Ephedrine
    • Norpseudoephedrine
    • Monadifil
    • Methylfenidate
    • Dexmethylfenidate
  • Reuptake inhibitors
    • Cocaine
    • TCAs
    • SSNRIs, SNRIs, ...
  • MAO inhibitors

B. Alpha agonists:

  • Alpha1 agonists
    • Phenylephrine
    • Methoxamine
    • Midodrine
  • Alpha2 agonists
    • Clonidine
    • Guaficine, guanabenz
    • Methyldopa
    • Demedetomidine
    • Tizanidine

C. Drugs acting on imidazoline receptors:

  • Moxonidine, Rilmenidine

11

11. Alpha-receptor antagonists

A. Alpha blockers:

  • Mechanism of action
  • Major uses
  • Non-selective alpha blockers
    • Phenoxybenzamine
    • Phentolamine
    • Tolazoline
    • Ergot alkaloids
  • Selective alpha1 blockers
    • Prozasin, doxazosin, terazosin
    • Alfusosin, tamsulosin, terazosin
    • Urapidil
    • Labetalol, carvedilol
  • Selective alpha2 blockers
    • Yohimbine
    • Mirtazepine

12

12. Beta-receptor antagonists

A. Characteristics of beta blockers:

  • Major consequences
  • General uses
    • Prolong survival
    • Centra indications
  • Adverse effects
  • Major differences
    • Route of elimination
    • Selectivity
    • Intrisinc sympathomimetic activity (ISA)
    • Lipid solubility
    • Additional actions on ion channels
      • Na+ blockade
      • K+ blockade
    • Additional vasodilatory action
    • Half-life
  • Contraindications

B. Drugs:

  • Beta1-cardioselective
    • Acebutolol
    • Atenolol
    • Betaxolol
    • Bisprolol
    • Celiprolol
    • Esmolol
    • Metoprolol
    • Nebivolol
  • Beta2-selective
    • Butoxamine
  • Mixed antagonists
    • Carvedilol
    • Labetolol
  • Non-selective
    • ​Carteolol
    • Nadolol
    • Penbutol
    • Pindolol
    • Propanolol
    • Sotalol
    • Timolol

13

13. Centrally acting skeletal muscle relaxants (spasmolytics). Dantrolene. Botulinum toxin

A. Spasms:

  • Definition

B. Spasmolytics:

  • Baclofen
  • Diazepam
  • Tizanidine
  • Tolperisone

C. Acute muscle spasms:

  • Mephenesin
  • Guaiphenesin
  • Chlorzoxazone
  • Carisoprodol

D. Direct-acting muscle relaxants:

  • Dantrolene
  • Botulinum toxin

14

14. Skeletal muscle relaxants acting on the neuromuscular junction

A. General:

  • Characteristics and actions
  • Clinical use
    • Presynaptic acting drugs
    • Post-synaptic acting drugs

B. Non-depolarizing (competitive antagonists of Nm):

  • Administration
  • Drugs
    • Isoquinolines
      • ​D-tubocurarine
      • Mivacarium
      • Cistracurium
      • Atracurium
      • Doxacurium
    • Steroids
      • ​Vercuronium
      • Rocuronium
      • Pancuronium
      • Pipecuronium
  • Pharmacokinetics
  • Pharmacodynamics
    • Order of curare induced paralysis
    • Mechanism of action
    • Selectivity
    • Factors influencing effect
    • Termination of the effect
  • Therapeutic uses
  • Adverse effects

C. Depolarizing (non-competitive agonist of Nm) - succinylcholine:

  • Administration
  • Pharmacokinetics
  • Pharmacodynamics
    • Order of curare-induced muscle paralysis
    • Mechanism of action
  • Therapeutic uses
  • Adverse effects

15

15. Selective beta2 -stimulants and other bronchodilators

A. Levels of asthma and targeted therapy:

  1. ​Mild intermittent
    1. Inhaled SABA
  2. Mild persistent
    1. Small dose inhaled steroids
  3. Moderate persistant
    1. Small dose inhaled steroids
    2. LABA
  4. Severe persistant
    1. Medium/high dose inhaled steroids 
    2. LABA

B. Beta2-agonists:

  • Non-selective beta2-agonists
  • SABA
    • Characteristics
    • Action
    • Adverse effects
    • Drugs
      • Albuterol (salbutamol)
      • Levalbuterol
      • Terbutaline
      • Fenoterol
  • LABA
    • ​Characteristics
    • Action
    • Adverse effects
    • Drugs
      • Salmeterol
      • Formoterol
      • Clenbuterol
      • Bambuterol
      • Idacaterol, Olodaterol, vilanterol

C. Other bronchodilators:

  • Xanthines
    • Theophylline
      • Therapeutic effect
      • Adverse effects
      • Pharmacokinetic
      • Clinical use
  • mAChR antagonists
    • Mechanism of action
    • Therapeutic effect
    • Clinical use
    • Adverse effects
    • Drugs
      • Atropine
      • Ipratropium
      • Tiotropium, glycopyrronium, aclidiunium, umeclidinium

16

16. Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants

A. Antiinflammatory agents:

  • Glucocorticoids
    • Effect
    • Mechanism of action
    • Clinical use
    • Routes of administration
    • Adverse effects
      • Contraindications
  • Inhaled corticosteroids
    • Drugs
      • Beclemethasone, propionate
      • Budesonide
      • Fluticasone
      • Ciclenoside
    • Therapeutic effect
    • Problems
    • Adverse effects
    • Clinical use
  • Leukotriene modifiers
    • Mechanisme of action
    • Effects
    • Pharmacokinetics
    • Clinical use
    • Drugs
      • Zafirlukast
      • Montelukast
      • Zileuton
  • Degranulation drugs
    • Cromolyn, nedocromil
  • Monoclonal antibodies
    • Omalizumab
    • ​Reslizumab
  • Other options
    • ​H1 receptor antagonist
    • PDE4 inhibitors
    • Desensitization
    • Antibiotics, oxygen

B. Antitussive:

  • Centrally acting
    • ​Opioids
      • Codeine
      • Dihydrocodeine
      • Narcotine
      • Ethylmorphine
    • Non-opioid
      • Butamirate
      • Dextrometorphan
  • Peripherally acting
    • Prexdiazine
    • Levodopropizine
    • Local anesthetics
    • Secretolytic expectorants

C. Expectorants:

  • Secretolytics:
    • Action
    • Drugs
      • Ipacacuanha
      • Saponines
      • Guajacol
      • Guaifenesin
      • Essential oils
      • Ammonium chloride
      • Iodine salts
  • Mucolytics
    • ​Action
    • Drugs
      • Bromhexine
      • Ambroxol
      • Acetylcysteine
      • Erdosteine
      • Carbocystenie
      • Dornase alpha
  • Secretomotoric agents - Ciliary activity
    • ​Action
    • Drugs
      • Beta2 agonists
      • Theophylline
      • Bromhexine, ambroxol
      • Essential oils
      • Acetylcysteine