Test 1 Flashcards
Pharmacodynamics
What a drug does to the critter
Pharmacokinetics
What the critter does to the drug
Pharmacokinetics: LADME
Liberation Absorption Distribution Metabolism Elimination
Two categories of drug administration
Enteral
Parenteral
Additive interaction
1+1=2
Synergistic reaction
1+1=3
Potentiation reaction
1+0=3
4 types of receptors
Regulatory proteins
Enzymes
Transport proteins
Structural proteins
3 aspects of drug receptor function
- Receptors determine the nature and characteristics of the drug concentration response curve
- Receptors function as regulatory proteins and part of chemical signaling mechanisms that provide targets for drugs
- Receptors determine the therapeutic and toxic effects of drugs on a critter
4 transmembrane signaling mechanisms
Ligand gated ion channels
G protein coupled receptors
Enzyme linked receptors
Intracellular receptors
How can differences in potency be overcome?
Giving more drug
Which is more important, potency or efficacy?
Efficacy
Therapeutic index
TD50/ED50
Toxic effect in 50% of population vs. therapeutic effect in 50%
Dangerous therapeutic index
<2
Definition of bioavailability
Fraction of administered drug that reaches systemic circulation
First pass metabolism
Via portal circulation
Liver metabolizes drugs limiting their bioavailability
Drugs with high first pass metabolism must be given in high doses orally or parenteral lay
Solubility characteristics of drugs
Too lipopholic: poorly absorbed
Too hydrophilic: difficulty passing through cell membranes
MOST COMMONLY ADMINISTERED DRUGS ARE WEAKLY ALKALINIC OR ACIDIC
Factors affecting bioavailability
Chemical stability in the GI tract
Drug formulation
3 factors affecting volume of distribution
Blood flow
Water/fat solubility
Protein binding
Major factor affecting sieving coefficient
Degree of protein binding
Volume of distribution calculation
Vd=D/Co
Dose/concentration
5 main ways to eliminate drugs
Urine Bile Hepatic metabolism Lung/oxygenator expiration Artificial filtration (hemoconcentrator)
Half life: 3.3, 4.3, and 4.3 years
- 3: 90%
- 3: 95%
- 3: 97.5%
Clearance rate equation
Cl= (0.693*Vd)/half life
Loading dose equation
LD= (Vd*target plasma concentration)/bioavailability
Maintenance dose equation
MD= (Clearance rate *target plasma concentration)/bioavailability
Two phases of biotransformation
Phase 1: metabolizes drug into more polar form
Phase2: conjugates drug with a chemical (acetylation)
Complex Liver biotransformation drugs through
Cytochrome P450 complex
Somatic nervous system transmission
One junction system travels via single nerve axon
Neurotranmitter: ACh
Autonomic nervous system
Extensive use of feedback arcs
Uses electrical impulses and neurotransmitters
Definition of ganglion
Nerve cell that lies outside the CNS
Preganglionic neurotransmitter
Acetylcholine for both PNS and SNS
3 divisions of the ANS
Parasympathetic
Sympathetic
Enteric
2 semiautonomous parts of the enteric division
Myenteric plexus (plexus of Auerbach) Submucous plexus (plexus of Meissner)
3 organs only recieving specifically sympathetic stimulation
Pilorector muscles, sweat glands, adrenal medulla
Types of receptors for cholinergic neurons
Nicotinic or muscarinic
Receptors for adrenergic neurons
Alpha
Beta
Dopaminergic
1 cardiovascular variable your body seeks to auto regulate
MAP
Net effect of Levophed
Increase SVR
Decrease HR
(Even though positive chronotrope)
Only location for muscarinic receptors
Effector postsynaptic cells of the PNS
Nicotinic receptor location
Neuromuscular junctions and ganglia of ANS
Rate limiting step for synthesis of ACh
Uptake of choline
Anesthetic adjuncts
Neuromuscular blockers
Antimuscarinic uses
Symptomatic bradycardia, pulseless electrical activity, AV block
Other Clinical use: adjunct Parkinson’s disease, motion sickness, eye exams, GI hyper motility, urinary incontinence
Side effects of antimuscarinics
Hot, dry, red, crazy
Tachycardia
Effects of Ganglionic blockers
Profound hypotension
Profound constipation
Major drug interactions for nondepolarizing neuromuscular blockers
Antagonized by acetylcholinesterase inhibitors
Synergistic with Ca channel blockers
Synergistic with halogenated hydrocarbon gas anesthetics
SUX side effect with psuedocholinesterase deficiency
Prolonged apnea
Most common in Persian Jews and Indian Hindu
Major SUX side effect
Hyperkalemia
Main SNS neurotransmitter
Norepinephrine
Rate limiting step of adrenergic neurotransmission
Tyrosine transported intracellularly and hydroxylated into DOPA
Most common method to get rid of norepinephrine
Reabsorption by presynaptic membrane
Alpha1 receptors have a high affinity for
Norepinephrine
Alpha2 receptors have a high affinity for
Clonidine (Catapres)
Alpha1 works on…
Smooth muscle of noncardiac organs
Eyes, bladder, and prostate
Apha2 use in cardiac surgery
Sedative as part of multimodal anesthesia
Epinephrine effect on SBP and DBP
Increase SBP
decrease DBP
Norepinephrine effect on SBP and DBP
Increased SBP
Increase DBP
DOC for cardiogenic or septic shock
Dopamine
DOC for struggling to come off bypass
Dobutamine
Isoproteronol effect on SBP and DBP
Same SBP
Greatly decreased DBP
Phenylephrine effect on SBP and DBP
Increases SBP
Increases DBP
Drug very commonly used in adult perfusion to increase SVR / arterial pressure
Phenylephrine (Neo)
4 privileged sites
Brain
Eye
Testicle
Fetus
Drug causing epinephrine reversal
Phentolamine
5 perfusion relevances for beta blockers
- MI
- Long term management of stable angina
- Hypertension
- Migraine headaches
- Hyperthyroidism and thyroid storm
5 Beta blocker side effects
- Bronchoconstriction
- Arrhythmias
- Hypoglycemia
- Drowsiness
- Sexual dysfunction