First Aid: Pharmacology Flashcards
Formula for loading dose
Cp x Vd / F
Formula for maintenance dose
Cp x CL x T / F
Which drugs have zero order elimination?
PEA = Phenytoin, Ethanol and Aspirin(at high dosages)
What is the acid base equation?
KA = [H][A-]/[HA] pKa = pH + log([HA]/[A-])
What type of reactions constitute Phase I metabolism? Who looses it?
Reduction, Oxidation, Hydrolysis with Cyt P450. Old people loose it.
What type of reactions constitute Phase II metabolism?
Conjugation: Glucoronidation, Acetylation, Sulfation. Old people have GAS. Slow acetylators have more side effects from drugs.
Efficacy versus Potency
Efficacy = Maximal Effect Potency = Less concentration needed to achieve the same effect.
What is the mechanism of action of ketamine?
Non-competitive NMDA antagonist
What is the therapeutic index?
TD50/ED50 Where TD50 equals the median dose at which people had toxic effects and ED 50 equals the median dose at which people had therapeutic effects.
The entire sympathetic nervous system is innervated by adrenergic neurons except…
the adrenal medulla and sweat glands which are innervated by cholinergic neurons and have M receptors.
What are the two nicotinic receptor subtypes and where are they found?
N_N found in autonomic ganglia and N_M found in NMJs. Both are Na channels.
What G protein subclass are alpha1 receptors and what is their function?
Gq
Vasoconstriction, Mydriasis, Sphincter contraction (GI & GU)
What G protein subclass are alpha2 receptors and what is their function?
Gi
Presynaptic receptor that decreases sympathetic tone. Decrease insulin and lipolysis. Increase platelet aggregation.
What G protein subclass are beta1 receptors and what is their function?
Gs
Increase HR, heart contraction, renin release, and lipolysis
What G protein subclass are beta2 receptors and what is their function?
Gs
Bronchodilation, vasodilation, increase HR, contractility, lipolysis, insulin release, and decrease uterine tone, promote ciliary muscle relaxation and increase humor production.
What G protein subclass are M1 receptors and what is their function?
Gq
CNS and Enteric nervous system
What G protein subclass are M2 receptors and what is their function?
Gi
Decrease HR and contractility of atria
What G protein subclass are M3 receptors and what is their function?
Gq
Increase exocrine gland secretion, gut peristalsis, bladder contraction, bronchoconstriction, and miosis
What G protein subclass are D1 receptors and what is their function?
Gs
Relaxes renal vascular smooth muscle
What G protein subclass are D2 receptors and what is their function?
Gi
Modulates transmitter release in the CNS
What G protein subclass are H1 receptors and what is their function?
Gq
Increase mucus production and vascular permeability. Bronchocontraction, pruritus and pain.
What G protein subclass are H2 receptors and what is their function?
Gs
Gastric acid secretion
What G protein subclass are V1 receptors and what is their function?
Gq
Increase vascular tone
What G protein subclass are V2 receptors and what is their function?
Gs
Increase H2O permeability for reabsorption in collection ducts
Which receptors belong in the Gq class and what is their downstream signal?
HAV 1 M & M (H1, alpha1, V1, M1 & M3)
Gq -> Phospholipase C -> DAG and IP3
DAG-> PKC
IP3 -> Ca -> Smooth muscle contraction
Which receptors belong in the Gs class and what is their downstream signal?
beta1, beta2, D1, H2 & V2
Gs -> Adenyl Cyclase -> cAMP -> PKA
PKA -> Ca in the heart
PKA -l Myosin Kinase
Which receptors belong in the Gi class and what is their downstream signal?
MAD 2s (M2, alpha2, & D2)
G1 -| Adenyl Cyclase -> cAMP -> PKA
Essentially opposes Gs
What is the mechanism of action of vesamicol?
Inhibits the uptake of cytosolic ACh into vesicles.
What is the mechanism of action of hemicholinium?
Inhibits ACh reuptake from synapse.
What is the mechanism of action of metyrosine?
Inhibits conversion of tyrosine to DOPA
What is the mechanism of action of amphetamines?
They get into the presynaptic Dopamine vesicles and inhibit the VMAT transporter. They also increase the pH and shut down the H+ transporter allowing Dopamine to diffuse out. In the cytosol they inhibit MOA and they reverse the action of the re-uptake DAT. This ultimately causes dopamine to be released.
Which four drugs inhibit re-uptake in the noradrenergic synapse?
SNRI, Amphetamines, TCAs, and Cocaine
What are the four direct cholinomimetics?
Bethanechol, Carbachol, Pilocarpine & Methacholine
What is bethanechol used for?
Ileus (neuro or post-op) and Urinary retention. Bethany call me maybe if you want to activate your bowel and your bladder.
What is carbachol used for?
Glaucoma & Pupillary Constriction
What is pilocarpine used for?
Increases sweat, tears and saliva (make your PILO wet). Used for glaucoma.
What is methacholine used for?
Diagnosis of asthma. (If it gets worst.)
What are the acetylcholine esterase inhibitors?
All the drugs that end in -stigmine plus edrophonium, donepezil & galantine.
What is neostigmine used for?
Ileus, post-op reversal of NMJ block, myasthenia gravis and urinary retention.
What is pyridostigmine used for?
Myasthenia gravis. (Get RID of MG)
What is physostigmine used for?
Atropine poisoning. BBB crossing.
What is donepezil used for?
Alzheimer’s Disease
What is edrophonium used for?
Myasthenia gravis diagnosis.
What are the symptoms of AChE inhibitor poisoning?
DUMBBELLS (Treat with atropine) D = Diarrhea U = Urination M = Miosis B = Bronchospasm B = Bradycardia E = Excitacion of muscle L = Lacrimation S = Sweating S = Salivation
Which muscarinic antagonist is used to treat Parkinson?
Benztropine “I Park my Benz”
Which muscarinic antagonist is used to treat motion sickness?
Scopolamine, which has CNS activity
Which muscarinic antagonist is used to treat COPD or Asthma?
Ipratropium (I pray I can breath) & Tiotropium
What are the effects of atropine on the following organs? Eye Airway Stomach Gut Bladder
Eye = Mydriasis & Cycloplagia Airway = Bronchodilation Stomach = Decrease acid production Gut = Decrease motility Bladder = Decrease urgency
Which muscarinic antagonist is used to treat urinary frequency?
Oxybutynin, Darrifenacin or Solifenacin
What is the selection profile of epinephrine and what is it used for?
beta > alpha
Anaphylaxis, Open angle glaucoma, asthma and hypotension.
What is the selection profile of Norepinephrine and what is it used for?
alpha1 > alpha2 > beta1
Hypotension (beware is decreases renal perfusion)
What is the selection profile of isoproterenol and what is it used for?
beta1 = beta2
ECG evaluation or tachyarrythmia
What is the selection profile of dopamine and what is it used for?
D1 = D2 > beta > alpha
Low dose to increase renal flow.
High dose dopamine for shock because it faso constricts, it is inotropic and chronotropic. (First line)
What is the selection profile of Fenoldopam and what is it used for?
D1 partial agonist only.
So it is used to treat HTN slowly by increasing GFR and decreasing resistance.