Term
| What are the two key components to the drug response curve? |
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Definition
| The Drug and the receptor. |
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Term
| What are the three types of Antagonists? Name them? Hint: PCP |
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Definition
Pharmacological-blocks at receptor Chemical-one drug deactivates another Physical-drugs with opposite effects block at different receptors. |
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Term
| What are the two key components to the dose response curve? |
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Definition
| The drug and the response (receptos-coupling action) |
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Term
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Definition
| First Plasma, then Protein, then Fat, skeletal muscle, etc. Someone with hypoalbuminemia wont have binding with higher circulating drugs. |
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Term
| Explain Up/Down Regulation. |
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Definition
| The body's response to drugs via creating more or less receptors. (e.g. a person on B-blockers a long time they will eventually no longer work as well) |
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Term
| What are the two components of the concentration/response curve. |
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Definition
| The relationship between the drug and the clinically observed response. |
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Term
What is the Threshold? What is the Hyperbolic State? |
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Definition
Threshold-Minimum Dose for Pharmacological Response Hyperbolic State- The top of the curve where you are maxxed out! (flatline) |
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Term
| What is an unusal response called? What usually causes it? |
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Definition
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Term
Henderson Hasselbach for acidic: for basic: |
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Definition
Acidic: Ionized/Unionized Basic: Unionized/Ionized |
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Term
What are some of the factors effecting absorption? Hint: BCCSR |
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Definition
| Bioavailability, Concentration, Circulation, Surface Area, Route of Administration |
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Term
| What is the Volume of Distribution Equation? |
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Definition
Dose of Drug / Plasma Concentration |
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Term
| What happens in Phase I of Biotransformation? |
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Definition
| Makes drugs more water soluable, Hydrolysis, oxygenation, reduction. |
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Term
| What happens in Phase two of Biotransformation? |
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Definition
| Conjuation of drug with endogenous substance (e.g. acetate or sulfate) for excretion |
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Term
| An inrease in meatbolism will have what effect on a drug? |
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Definition
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Term
| What kind of drugs can be filtered in the glomerulus? |
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Definition
| UNbound drugs-metabolites can filter back and forth in the proximal and distal tubules. |
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Term
| in regards to elimination, acidic urine gets rid of..... |
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Definition
| promotes elimination of bases.... |
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Term
| What is the formula for clearance/excretion? |
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Definition
| rate of elimination/drug concentration in body |
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Term
| Explain Capacity eliminated (zero order) elimination |
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Definition
A constant amount of drug is eliminated over time REGARDLESS of concentration e.g. Alcohol 10 mg/hr |
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Term
| What is First Order Clearance? |
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Definition
| A known/predicted amount is eliminated per unit of time. (e.g 50% hour) |
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Term
| In hepatic extraction with low blood flow will you have higher or lower extraction? |
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Definition
Higher extraction (inversley related) Conveyor Belt Theory |
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Term
| As Elimination increases what happens to half-life ? |
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Definition
| Half life will decrease becase more drug is being eliminated. |
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Term
What diseases can contribute to decreased liver blood flow with a decreased extraction ratio? |
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Definition
Liver and Cardiac Disease Portal HTN., cirrhosis |
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Term
| Explain Distribution Half Life |
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Definition
| The Initial Fall in concentration, it describes the rapid process of drug distribution from central to peripheral compartments |
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Term
| Explain Elimination Half-Life |
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Definition
After distribution, the time it takes for for the drug to dissapear from by irreversible elimination from central compartment |
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Term
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Definition
The time to reach a steady state is related to t(1/2) concentration to reach 94% in 4 half lives |
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Term
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Definition
| Amount Administered=Amount Eliminated |
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Term
| Context Sensitive Half-time |
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Definition
| The time necessary for plasma concentration to decrease 50% after infusion discontinued |
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Term
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Definition
| Dose regimen to produce desired effect |
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Term
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Definition
| maintain steady state and dose to replace eliminated drug |
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Term
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Definition
| steady state to = rate of elimination |
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Term
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Definition
| Needed to make a steady state in a drug with a long half-life |
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Term
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Definition
| At a steady state, drug concentrations fluctuate (peak and trough) |
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Term
Name the 5 types of Transmembrance Signaling hint (GILTR 2) |
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Definition
G-Proteing Ion Channel (ligand-gated) Lipid Soluable Ligand Transmembrance Receptor Protein 2nd Messengers |
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Term
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Definition
| e.g. NO2 signals guanylate cyclase to produce cGMP and causes vasodilation |
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Term
| What drug binds to the DNA in the nucleus |
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Definition
| steroids- to stimulate gene transcription |
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Term
| Transmembrane Receptor Protein |
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Definition
Intracellular enzymatic activity regulated by an extracellualr site e.g. Lidocaine blocks Na+ channel hyperpolarizes cell.....it can't depolarize for an action potential or Insulin binding to sugar |
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Term
| Ligand gated transmembrane Ion Channel |
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Definition
Receptors are: GABA, Ach, etc receptors transmit signals increasing ion conduction and alters electrical potential difference Ach opens nicotinic Ach channel, allows Na+ influx, and causes exitatory or GABA lets Cl- in to make inhibitory response |
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Term
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Definition
| Transmembrane receptor protein stimulates a GTP binding cell surface detects, activates G protein stimulates an enzyme OR ion channel and 2nd messenger (cAMP, IP3, CA2+) |
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Term
| What is a serpentine receptor |
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Definition
| Describes how the receptor spans the membrane |
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