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Exam 2 Material
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22
Pharmacology
Graduate
03/24/2015

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Term
How Well Does a Drug Get Into the CNS?
(Optimal Passive Factors)
Definition
Highly lipid soluble
Low molecular weight
Non-polar
Alkaline pKa
Low protein binding
Oily drugs
Term
CNS Efflux Proteins
(MDR1)
Definition
Prevent high concentration of drug in the brain; kick out bad drugs and substrates like bouncers.
Term
Neuronal Drug Targets
Definition
1) Synthesis and storage of Neurotransmitter
2) Action potential traveling neuron
3) Membrane depolarization activates voltage sensitive calcium channels
4) Vesicle fusion with snare proteins
5) Post synaptic Binding
6) Ligand is removed from receptor
7) Ligand enzymatically metabolized in cleft
8) Ligand recycled back into pre-synaptic cell.
Term
Tachyphylaxis
Definition
Rapid appearance of progressive decreas in response to a given dose after repetitive administration of a pharmacologically or physiologically active substance.
Term
Poison Center #
Definition
1-800-222-1222
Term
Paracelsus
Definition
"Poison is in everything and nothing is without poison. The dosage makes it either a poison or a remedy.
Term
Type 1: Immediate-type hypersensitivity
- Most Important -
Definition
Trigger: Antigen-binding on IgE on mast cells
Mediators: Histamine and serotonin
Signs and symptoms: hives, urticaria (a kind of skin rash notable for pale red, raised, itchy bumps), bronchoconstriction, hypotension, and shock.
Extra: Immediate and deadly; after more and more exposure, the worse the reaction is and may experience anaphylaxis.
Term
Type 2: Antibody-dependent cellular cytotoxicity (Humoral)
Definition
Trigger: IgG and complement binding cell-bound antigen.
Mediators: Neutrophils, macrophages, and NKCs
Signs and symptoms: Hemolysis
Term
Type 3: Immune-complex disease (Humoral)
Definition
Trigger: IgG and complement binding soluble antigen
Mediators: neutrophils, macrophages, NKCs, reactive oxygen species, and chemokines.
Signs and symptoms: cutaneous vasculitis
Term
Type IV: Delayed-type hypersensitivity (Cell-mediated)
Definition
Trigger: antigen in association with MHC protein on the surface of APCs
Mediaotrs: Cytotoxic T lymphocytes, macrophages, and scytokines
Signs and symptoms: muscular rashes and organ failure
Term
Acetaminophen Toxicity
Definition
Leading cause of liver failure in Us
* Narrow safety margin
- 4g/day max dosage
* Acute overdoes from greater than or equal to 7g or 150mg/kg: causes GI pain and N/V early and transitions to bleeding, acidosis, and liver failure later.
Term
Hydrocone Toxicity
Definition
Widely available and abused, tirggers opiate receptors.
* Warnings include: hepatotoxicity, respiratory depression, misuse, abuse, and diversion.
* Acute overdose: sedation, respiratory depression, pinpoint pupils, constipation, hypotension and bradycardia.
* Antidote: naloxone; opiate antagonist by blocking receptor, rapid onset and short-acting.
Term
SERT
Definition
Transporter for 5HT reuptake
Term
NET
Definition
Transporter for NE uptake
Term
SSRI
Definition
Prevents reuptake of 5HT only (agonist), blocks the reuptake of serotonin leading to increased concentrations in the synaptic cleft
Term
SNRI
Definition
Prevent reuptake of 5HT and NE (agonist)
- involves the blockade of 5-HT and norepinephrine reuptake in a concentration-dependent manner.
Term
SNRI's
Definition
Venlafaxine, Duloxetine
Term
SSRI's
Definition
Fluvoxamine
Term
Migraine Headache
Definition
Primary dysfunction: no well-defined structural causes.
- Carries a vascular component (dilation) and a neuron hyper-excitability component within the occiptal cortex
- Unilateral (pain on one side, visual aura precipitates (see/feel the headache coming, ex. see a light), throbbing character associated with photosensitivity, lethargy, N/V, diaphoresis, inability to concentrate
Term
Serotonin syndrome
Definition
Occurs when you take medications that cause high levels of the chemical serotonin to accumulate in your body.
*Severe Symptoms: High fever, Seizures, Irregular heartbeat, Unconsciousness.
*Symptoms: Agitation or restlessness
Confusion
Rapid heart rate and high blood pressure
Dilated pupils, Loss of muscle coordination or twitching muscles
Muscle rigidity, Heavy sweating, Diarrhea,Headache, Shivering, Goose bumps
Term
Migraine Drugs
(5HT-1b)
Definition
Inhibit the second messenger of 5HT, decreases cAMP, works on the presynaptic neuron, serotonin agonists that reverse the dilation of the blood vessesl in the brain (causes restriction of blood vessels)
Term
Catecholamines
Definition
Epinephrine, Norepinephrine, Dopamine
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