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Quiz 2
PDA
59
Pharmacology
Professional
10/31/2011
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Term
o Group 1
 Definition
Protein therapeutics with enzymatic or regulatory activity
Term
 Group 1a
 Definition
Replace a protein which is deficient or abnormal


• Factor VIII
• Insulin and its analogues
• Growth Hormone
Term
 Group 1b
 Definition
Augment an existing pathway


• Erythropoietin
• Pegylated interferon
• Tenecteplase
Term
 Group 1c:
 Definition
Provide a novel function or activity


• Collagenase
• L-asparaginase
• Etanercept
Term
o Group 2
 Definition
Protein therapeutics with special targeting activity
Term
 Group 2a
 Definition
Interfering with a molecule or organism by binding to it and blocking its function or targeting it for degradation

• Abciximab

• Enfuviritide
• Infliximab
Term
 Group 2b
 Definition
Stimulating a signalling pathway

• Trastuzumab
Term
 Group 2c
 Definition
Delivering other compounds or proteins

• Gemtuzumab ozagamicin
Term
o Group 3
 Definition
Protein vaccines
Term
 Group 3a
 Definition
Protecting against a deleterious foreign agent


• HBsAg
• Lyme disease (Borrelia burgdorfei)
Term
 Group 3b
 Definition
Treating an autoimmune disease

• Anti-Rh IgG
Term
 Group 3c
 Definition
Treating cancer

• Currently in clinical trials
Term
o Group 4:
 Definition
Protein diagnostic


 HIV antigens
 Hepatitis C antigens
 Thyroid stimulating hormone (TSH)
 Glucagon
Term
Sympathetic preganglionic neurons
 Definition
arise in the ventral horn of the thoracic and lumbar segments of the spinal cord and project onto postganglionic neurons in the paravertebral and prevertebral ganglia.
 Sympathetic postganglionic neurons innervate many organs, including smooth muscle.
• The adrenal medulla is innervated by preganglionic neurons of the sympathetic nervous system
Term
Parasympathetic preganglionic neurons
 Definition
arise in nuclei in the brainstem/sacral segments of the spinal cord and project onto postganglionic neurons in ganglia located near the innervated organs.
Term
Parasympathetic
 Definition
 Pharmacological M-agonist bethanecol (GI and urinary tract motility)
 M-antagonist atropine (dilate pupils/ increase heart rate) action
Term
Sympathetic
 Definition
 Albuterol (B2 agonist) dilate bronchioles selectively vs.
 Metroprolol (B2 antagonist) selectively decrease heart rate
Term
 Neostigmine
 Definition
(agonist of NMJ) increase skeletal muscle stimulation (Myasthenia gravis treatment)
Term
 Pancuronium
 Definition
(antagonist of NMJ) induces paralysis
Term
o Acetylcholine
 Definition
 parasympathetic and somatic neuromuscular junctions.
 Few sympathetic neuroeffector junctions; sweat glands and vasodilator fibers in skeletal muscle.
 lack of specificity of drugs acting on acetylcholine neurotransmission
Term
o Norepinephrine/ Ephinephrine
 Definition
 Norepinephrine (noradrenaline) - Primary neurotransmitter at most sympathetic postganglionic neuroeffector junctions,
 Epinephrine (adrenaline) is the principal catecholamine released from the adrenal medulla
Term
o Other neurotransmitters
 Definition
 autonomic nerves of the GI tract, genitourinary tract and certain blood vessels.
 neuropeptide Y, vasoactive intestinal polypeptide, enkephalin, substance P, serotonin, adenosine triphosphate, and nitric oxide.
Term
Musacarinic Receptors
 Definition
o Parasympathetic neuroeffector junctions
o M1-M5 human GPCR – G-Protein Coupled Receptor
 M3 receptor- smooth muscle contraction and gland secretion.
 M2 receptor- mediates cardiac slowing
 M1 receptor -modulation of neurotransmission at central and peripheral sites.
o Activation in skeletal muscle causes muscle contraction.
o M1, M3 and M5 stimulation of PLC, IP3 and DAG
o M2 and M4 inhibition AC and K+ channel activation
o Hyperpolarization of the cell
o Latency 100-250 ms
Term
Nicotinic receptor action
 Definition
o Found in all autonomic ganglia (Nn neuron Nm muscle)
o NN –Neuronal- excites neurotransmission
o NM –somatic neuromuscular – excites muscle contraction
o NM:5 subunits; 30-50% homology
o NN:  and  subunits
Term
Nicotinic receptor structure biology
 Definition
o 2 subunit - hydrophobic pocket serves as binding site for Ach agonist
o Predominant ion in nAChR is Na+,
o Net inward Na+ current depolarize the cell
o Brief latency <10ms
Term
Synthesis of Achetylcholine
 Definition
o Choline sources:
 Synaptic Cleft
 Plasma based (lipid phosphatidylcholine)1
 Phospholipids (phosphorylcholine)
o Acetyl-CoA:
 Glycolysis (mitochondria)2
o Rate limiting steps of ACh: Choline uptake
 Low affinity facilitated diffusion (Km=10-100M)
 High affinity transport (Km=1-5M) 3
Term
Cholinergic Neurotransmission
 Definition
o direct-acting acetylcholine receptor agonists : bethanechol and pilocarpine,
o indirect-acting acetylcholine receptor agonists: cholinesterase inhibitors (physostigmine), increase the synaptic concentration of Ach.
o acetylcholine receptor antagonists:
o muscarinic receptor antagonists (atropine)
o nicotinic receptor antagonists /ganglionic blocking agents (e.g., trimethaphan) and neuromuscular blocking drugs (e.g., tubocurarine).
Term
Effects of Acetylcholine on M receptors
 Definition
o Eye iris
 contraction and miosis
o Salivary and lacrimal glad
 thin and watery secretions
o Heart
 Bradycardia
 Lower conduction velocity
 AV block in high doses
 Slight lower in contractility
Term
How does botulinum toxine cause muscle weakness and prolonged paralysis?
 Definition
o Degrades synaptobrevin and prevents the fusion of presynaptic storage vesicles with the cell membrane
Term
• A woman with facial muscle spasms is treated with an agent that inhibits the release of acetylcholine. Which side effect is most likely to occur in this patient?
 Definition
o Dry mouth
Term
Catecholamines
 Definition
 Norepinephrine (NE), the principal transmitter of most sympathetic postganglionic fibers
 dopamine (DA), the predominant transmitter of the extrapyramidal system, mesocortical and mesolimbic neuronal pathways
 epinephrine, the major hormone of the adrenal medulla
Term
The α1-adrenoceptors
 Definition
• mediate smooth muscle and glands contraction
Term
The α2-adrenoceptors
 Definition
• cause transmitter release, contraction
Term
Activation of β1-adrenoceptors
 Definition
• produces cardiac stimulation
Term
The β2-adrenoceptors
 Definition
• mediate smooth muscle relaxation
Term
Adrenergic Neurotransmition
 Definition
 Direct- acting adrenoceptor agonists - albuterol, epinephrine
 Indirect- acting adrenoceptor agonists
• Amphetamine(+), cocaine(-)
o Acts on reuptake of NE
• COMT or MAO inhibitors (primarily effects on CNS )
Term
phentolamine
 Definition
selectively blocks α-adrenoceptors
Term
propranolol
 Definition
selective β-adrenoceptors blocker
Term
 Inhibit synthesis of neurotransmitter
 Definition
• Hemicholinium
• Metyrosine (alpha-methyl-para-tyrosine)
Term
 Prevent vesicular storage of neurotransmitter
 Definition
• Vesamicol*
• Reserpine
Term
 Inhibit release of neurotransmitter
 Definition
• Botulinum toxin
• Bretylium
Term
 Increase release of neurotransmitter
 Definition
• Black widow spider venom (α-latrotoxin)*
• Amphetamine
Term
 Inhibit reuptake of neurotransmitter
 Definition
• Cocaine
Term
 Inhibit metabolism of neurotransmitter
 Definition
• Cholinesterase inhibitors (physostigmine)
• Monoamine oxidase inhibitors (phenelzine)
Term
 Activate postsynaptic receptors
 Definition
• Acetylcholine, bethanechol, and pilocarpine
• Albuterol, dobutamine, and epinephrine
Term
 Block postsynaptic receptors
 Definition
• Atropine and tubocurarine (block muscarinic and nicotinic receptors, respectively)
• Phentolamine and propranolol (block α- and β-adrenoceptors, respectively)
Term
o Epinephrine/Norepinephrine …?
 Definition
 Are released by adrenal medulla
pon binding to  2 adrenoceptors Ep cause smooth muscle relaxation
Term
o In a sympathetic postganglionic nerve ending which of the following blocks the conversion of an intermediate amino acid?
 Definition
 Metyrosine
Term
o Cerbral hemisphere
 Definition
 Cortex- site of action of many drugs
 Basal ganglia - intended actions , movement (PD)
 Limbic system: cingulate gyrus, Hippocampus, amygdala- emotions, social behaviour (AD)
Term
o Pharmcological modification of Brain regions
 Definition
 Barbiturates and Benzodiazepines hypnotic/sedetative agents potentiate the action of inhibitory neurotransmitters in cortex.
 Levodopa acts on the dopaminergic neurotransmission and ameliorates symptoms of Parkinson disease in striatum
 Drugs that affect limbic system (hippocampus) and cholinergic neurotransmittion are used in Alzheimers Disease
Term
o Neurotrasmitters in CNS
 Definition
 Exitatory (E, D)
 Inhibitary (G, GABA)
 Glutamate act on both ionotropic and metabotropic receptors
• Overactivation of glutamate receptors lead to ischemic brain injury (neuronal death)
• Felbamate
o used in treatment of refractory epilepsy
o inhibits NMDA receptors -> reduce excessive neuronal activity
 GABA acts on GABA receptors
• Barbiturates and benzodiazepines and potentiate the effect of endogenous GABA
Term
 Dopaminergic neurons
 Definition
• Subtantia niagra-control intended actions/ movements (PD –SN degeneration)
Term
 Noradrenergic neurons
 Definition
• Locus ceruleus- maintain vigilance, responsiveness to unexpected stimulus
• COCAIN- activate this system by inhibiting reuptake of norepinephrine – Hypervigilance
• TCA (antidepressant) blocks reuptake of NE
Term
 Serotonergic neurons
 Definition
• Brain stem (raphe nuclei) – modulating pain, regulate wakeness/ sleep
• Depression- dysfunction of seretonin system
• (SSRIs- used for treatment of depression)
Term
 Acetylcholine
 Definition
• Nucleus : Alertness/ sleep-awake cykle, AD
Term
 Histamine
 Definition
• Hypothalamus: forbrain arousal. Antihistamines
• (H1 receptor antagonist) used to treat allergies.
Term
o NITRIC OXIDE (NO):
 Definition
 Peripheral mechanism of action:
 Its released from nerves (nitrergic) innervating blood vessels and smooth muscles of the GI
 Endothelial cell–dependent mechanisms of relaxation including the coronary circulation.
 Activates specific GPCRs ->promotes NO production.
 activating GC-> cyclic GMP
 Nitrovasodilating act through conversion to or release of NO
 CNS mechanism of action:. NO is a small protein neurotransmitter
• Binds to receptors residing in the presynaptic neuron.
Term
o NEUROPEPTIDES
 Definition
 Endocrine, aoutocrine and paracrine effects
 Opioids, Tachykinins, Secretins, Insulines
 Piturary hormone release : CRH, GnRH, TRH, GRH
 Opioid receptors in the spinal cord and brain mostly involved in pain sensation: Pharmacological targets of analgesics (morphine) and drug abuse (heroin)
Term
o Blood Brain Barrier (BBB) permeability
 Definition
 Lipophilic substances, incl lipid soluble gases
• high w/o coefficient pass BBB
 Hydrophilic substances (glucose) pass BBB only with help of specific transporters
 Hexose transportes glucose
 3 transporters involved in the transport of amino acids (L-DOPA but not dopamine)
 Protection against toxic substances
• Multiple drug resistance transporters
• Metabolic BBB
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