Topics outline Flashcards

Question 1

Q

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

Answer

A

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

Question 2

Q

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

Answer

A

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

Question 3

Q

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

Answer

A

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

Question 4

Q

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

Answer

A

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

Question 5

Q

Cholinergic transmission and its presynaptic modification. Ganglion blocking agents.

Answer

A

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

Question 6

Q

Adrenergic transmission and its presynaptic modification

Answer

A

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

Question 7

Q

Cholinomimetics

Answer

A

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

Question 8

Q

Muscarinic receptor blocking drugs

Answer

A

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

Question 9

Q

Catecholamines

Answer

A

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

Question 10

Q

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

Answer

A

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

Question 11

Q

Alpha-receptor antagonists

Answer

A

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

Question 12

Q

Beta-receptor antagonists

Answer

A

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

Question 13

Q

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

Answer

A

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

Question 14

Q

Skeletal muscle relaxants acting on the neuromuscular junction

Answer

A

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

Question 15

Q

Selective beta2 -stimulants and other bronchodilators

Answer

A

A. Levels of asthma and targeted therapy:

Mild intermittent
1. Inhaled SABA
Mild persistent
1. Small dose inhaled steroids
Moderate persistant
1. Small dose inhaled steroids
2. LABA
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

Question 16

Q

Antiinflammatory agents used in bronchial asthma. Antitussive agents and expectorants

Answer

A

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

Brainscape's Knowledge GenomeTM

Topics outline Flashcards

Brainscape's Knowledge Genome^TM