Pharmokinetics
What is BA
The FRACTION of the administered dose of a drug that reaches the systemic circulation in ACTIVE form
Describe the affinity and efficacy for agonists, partial agonists, and antagonists. Also, name examples from class (3)
Partial: some affinity, lower efficacy (Buprenorphine)
Antagonist: high affinity, no efficacy (Nalaxone)When given SubL, will naloxone or Buprenorphine take affect first?'
When given through IV, will naloxone or Buprenorphine take affect first?
SubL - buprenorphine (since higher BA then)
IV - Naloxone (since higher BA then)
What are the types of nodes that Beta 1 targest
SA - chronotropic effect (increase HR). treats bradyc
AV - TWO TYPES2. Ionotropic effect (increase force of contraction). Treats decompensated heart failure.
List, from most BA to least BA
Options: IM, IV, SubC, SubL, Oral
IV, SubC (since more consistent over body), IM (since movement differs), SubL, Oral
What is steady state concentration in terms of rate of drug admin and rate of drug elim
Balance where drug intake equals drug elimination
In the presence of a full agonist, how will partial agonists behave?
(A) It will block the effect of the full agonist at the receptor
(B) It will increase the effect of the full agonist at the receptor
(C) It will have no effect of the full agonist at the receptor
(D) None of the above
(A) It will block the effect of the full agonist at the receptor
In the presence of a full agonist, acts as a competitive inhibitor and producing a lower response.
Where does sympathetic and parasympathetic originate
Parasym - brainstem or sacral
Which of the drugs, Phentolamine or Phenoxybenzamine, would be ideal for treating chronic hypertension? Why?
Phenoxybenzamine since noncompetitive and taken orally instead (metabolized longer)
Note that phentolamine is taken through IV
Name 4 factors that affect distribution of drug in body
Blood flow, protein binding, molecular size, lipid solubility
What ethnic group have polymorphisms leading to different alcohol metabolism
Leads to facial flushing (dilation of vessels), causing them to metabolize alcohol slower
What does transient phosphorylation relate to (up or down regulation) and what does it mean?
Down regulation.
Means effect does not last, and you have to keep dosing
What is the purpose of Muscarinic receptors in the Symp
Provides for interaction between parasym and sym.
The release of ach from parasym inhibits the release of NEP from sym.
This means that parasym can modulate and reduce the sym acitivty (maintain homeo)
For a patient with diabetes or asthma, would you prescribe a selective (Beta-1 or Beta-2 antagonist) or non-selective beta-blocker? Why?
Beta 1 antagonist preferred since increased heart rate makes it harder to diabetic patients to recognize when their blood sugar is low
Beta 2 antagonist would just cause more asthma
What is entero-hepatic cycling
Recycling of drug between liver and intestines
What is the difference between tolerance and addiction?
Think about Mr. Peteet and his coffee!!
Tolerance means receptors downregulate, need more for same effect, and withdrawal
Addiction (more of a social construct) means adverse effects based on use in life (interpersonal, legal, and financial)
What is the difference between what Km does for competitive and noncompetitive inhibition
Km decreases for competitive (decreased affinity)
Km does not change (since binding affinity stays the same, molecule just cant figure out how to bind)
What is anticholinergic toxidrome? How do you know if you have it?
Anti-muscarinic toxidrome
Produces anticholinergic effects since blocking ach receptors
Signs: hyperthermia, skin flushing, dry mouth, confusion, delirium, mydriasis, blurred vision, seizure, urinary retention, tachy
Agonism at which receptor is responsible for a decrease in norepinephrine release?
Alpha-1 adrenergic receptor
Alpha-2 adrenergic receptor
Beta-1 adrenergic receptor
Beta-2 adrenergic receptor
Alpha-2 adrenergic receptor
What is polymorphism and why it is important in terms of drug prescribing
Polymorphism in genes affects how patients process medications
Genetic variations (poor or ultrarapid CYP2D6)
Poor metabolizer cannot convert drug into active form, so no pain releif
Ultrarapid metabolizer converts drugs fast, which can lead to death
What is cross tolerance
Drugs that affect the same receptors
Tolerance of one drug reduces sensitivity to another drug, even if the second drug has not been used yet (similar MOA)
Dynamic - decreased affinity and downregulation (receptors level adaptations)
kinetics - absorption, distribution, metabolism, excretion. MENTIONING DRUG LEVELS
What is a curariform drugs? What are examples
Curariform - "Curari" was an arrow that africans used to paralyse their victims (think of avatar)
Nondepolarizing neuromuscular blockers (Pancuronium, Cisatracurium)
What is the primary and secondary (compensatory) processes of NEP, EP, Isoproterenol, Dopamine
EP. Primary: increase HR (beta 1) and vasodilation (beta 2). Secondary: Reflex tachy from vasodilation
Isoproterenol. Primary: Increase HR (beta 1) and vasodilation (beta 2). Secondary: Reflex tachy (NOTE SAME AS EP)
Dopamine. Primary: Increase HR (beta 1) and vasoconstriction (alpha 1). Secondary: Reflex brady