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Pharmacology summary notes. Unit 8. REB, 4MedStudents.com. 2003. Amino Acid Transmitter. Excitatory Neurotransmitter : Glutamate, Aspartate, Cysteic Acid, Homocysteic acid Inhibitory Neurotransmitter : GABA, Glycine, Alanin, Taurine. GABA Agonist : Muscimol GABA Antagonist : Bicuculline

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pharmacology summary notes

Pharmacology summary notes

Unit 8

REB, 4MedStudents.com. 2003

amino acid transmitter
Amino Acid Transmitter
  • Excitatory Neurotransmitter: Glutamate, Aspartate, Cysteic Acid, Homocysteic acid
  • Inhibitory Neurotransmitter: GABA, Glycine, Alanin, Taurine.
  • GABA Agonist: Muscimol
  • GABA Antagonist: Bicuculline
  • GABA Modulator: BDZ, Barbiturates, Steroids

Prof. Adem

sympathomimetics
Sympathomimetics
  • Direct acting drugs:
    • Epinephrine
    • Isoproterenol
    • Phenylephrine
  • Indirect acting drugs
    • Amphetamine
    • Tyramine
  • Mixed acting drugs:
    • Ephedrine
    • Metaraminol

Prof. Adem

adrenergic antagonist
α - Adrenergic Antagonist

Haloalkylamine derivatives:

Phenoxybenzamine

Used to treat pheochromocytoma

Imidazoline derivatives:

Phentolamine

Quinazoline derivatives:

Prazosin

  • All α Antagonists are not selective to α1 or α2, except Prazosin which is selective to α1
  • Therefore, all α Antagonists ( phenoxybenzamine & Phentolamine) causes tachycardia & postural hypotension. Except Prazosin has minimal side effects.

Prof. Adem

adrenergic antagonist5
β- Adrenergic Antagonist

Non Specific blocker ( α or β)

Labetalol

Used for hypertensive crisis with excess peripheral resistance

Non Selective β blocker (β1 or β2)

Propranolol, Timolol (used for chronic glaucoma)

Cardio-Selective Blocker (β2 only)

Atenolol (the only β blocker used for asthmatics

Partial Agonist

Acebutolol, Pindolol ( has intrinsic sympathomimetic effect

Prof. Adem

cholinomimetics
Cholinomimetics

Bethanechol

Carbachol

Pilocarpine

Used for emergency glaucoma

  • The drug that inhibit the transport of choline: Hemicholinium
  • The drug that inhibit the release of Ach: Botulinum toxin
  • The drug that induce the release of Ach: Spider venum

Prof. Adem

muscarinic antagonists
Muscarinic Antagonists

Atropine

Clinical uses:A belladonna alkaloid, antispasmodic agent, antidote for muscarinic agonists (and idirect agonists as acetylcholinesterase inhibitors) and antisecretory agent.

Side effects: dry mouth, tachycardia, blurred vision and constipation

Ipratropium

Scopolamine

Prof. Adem

choline esterase inhibitors

Dr.Petroianu

Choline Esterase Inhibitors
  • Central Nervous System Syndrome
  • Mad as a hatter
  • Red as a beet
  • Dry as a bone
  • Blind as a bat
  • Hot as a hear
  • Physostigmine is used coz it is the only drug act CNS receptors
  • Myasthenia
  • Pryidostigmin Act on peripheral receptors
  • Alzheimer’s Disease
  • Tacrine
  • Rivastigmine
  • Donepezil
  • Drug of choice:
  • less side effects
  • Long duration
  • Reversal NDMR
  • Edrophonium
  • Neostigmin
  • Act on peripheral receptors
non depolarizing muscle relaxants

Dr.Petroianu

Non Depolarizing Muscle Relaxants

Intermediate, metabolized by Hoffmann degrd.

depolarizing muscle relaxants sux
Depolarizing Muscle RelaxantsSUX
  • SUX is the ultra-short acting muscle relaxant, and has a rapid onset of action.
  • SUX is metabolized by AChE
  • Side effects of using SUX:
    • Fasciculation
    • Myalgia
    • pressure(intracranial, intragastric, intraoccular)
    • Similar to Ach ( Bronchospasm, Bradycardia)
    • Hyperkalemia
    • Masseter Muscle Spasm
    • Malignant hyperthermia

Dr.Petroianu

intravenous hypnotics

Dr.Petroianu

Intravenous hypnotics

NMDA Antagonist

Kitamine

The only hyponotic that have potent analgesic effect.

GABA Agonist

BDZ ex. Medazolam

Barbiturate ex. Thiopental which induce release of histamine.

Propafol

Etomidate which inhibit steroid synthesis.

inhaled anesthetics

Dr.Petroianu

Inhaled Anesthetics

GABA Agonist

Halothain metabolized by liver causing hepatitis

Enoflurain

Isoflurain

Sevoflurain

Desflurain no side effect but lipid solubility therefore dose.

NMDA Antagonist

Nitrous oxide

drugs acting on autonomic ganglia

Dr.Petroianu

Drugs acting on Autonomic ganglia

Nicotine

Non-selective

Trimethaphan

Short acting

Given I.V

Macamylamine

Long acting

Oral administration