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.
What is the selection profile of dobutamine and what is it used for?
beta1 > beta2 = alpha
Used in heart failure and has mostly inotropic effects.
What is the selection profile of phenylephrine and what is it used for?
alpha1 > alpha2
Hypotension, rhinitis and optho procedures (mydriasis)
What is the selection profile of albuterol and what is it used for?
beta2 > beta1
Acute asthma attacks
What is the selection profile of metaproterenol and what is it used for?
beta2 > beta1
Acute asthma attacks
What is the selection profile of salmeterol and what is it used for?
beta2 > beta1
Long term asthma or COPD management
What is the selection profile of terbutaline and what is it used for?
beta2 > beta1
It decreases uterine contractions in premature labor
What is the selection profile of ephedrine and what is it used for?
alpha = beta (it causes vesicle release)
Nasal decongestion, incontinence and hypotension
What is the mechanism of action of cocaine?
NE re-uptake inhibitor.
Compare the effects on mean arterial pressure and heart rate between NE and Isoproterenol.
With NE there is an alpha1 mediated increase in MAP with a reflex bradycardia. With Isoproterenol there is a beta2 vasodilatory effect and a beta1 and beta2 tachycardia.
What is the mechanism of action of clonidine and what is used for?
alpha2 agonist used for hypertensive urgency, ADHD, Severe pain, EtOH withdrawal, opioid withdrawal.
What is the mechanism of action of alpha-methyldoma and what is used for?
alpha2 agonist used for gestational hypertension.
What is the selection profile of phenoxybenzamine and what is it used for?
Non selective alpha blocker used for pheo. Can cause hypotension and reflex tachycardia.
What is the selection profile of phentolamine and what is it used for?
Non selective alpha blocker used for patients in a hypertensive emergency caused by tyramine ingestion while on MAO inhibitors. Also used for NE extraversion on IV sites.
What is the selection profile of prazosin, terazosin, and doxazosin and what is it used for?
alpha1 blockers used to relieve BPH symptoms. Prazosin is also used for PTSD. Can treat hypertension. Can cause orthostatic hypotension.
What is the selection profile of tamsulosin and what is it used for?
alpha1 blocker used to relieve BPH symptoms. Can cause orthostatic hypotension.
What is the selection profile of mirtazapine and what is it used for?
alpha2 blocker used for depression. Can cause sedation, increase in cholesterol and increased appetite.
What type of arrhythmia are beta blockers useful for and how do they work?
They decrease AV conduction velocity and can be used for SVTs.
What is the effect of beta blockers in the eye and what are they used for?
They decrease humor production. Timolol is used for glaucoma.
What are the toxicities of beta blockers?
Impotence Bradycardia AV block Seizures Sedation Dislipidemia (metoprolol) Worst asthma or COPD Unopposed alpha effect on cocaine users.
Which beta blockers are beta 1 selective?
Acetabutolol (partial agonist), Atenolol, Betaxolol, Esmolol, Metoprolol (all the ones from A to M)
Which beta blockers are non-selective?
Nadolol, Pindolol (partial agonist), Propanolol, Timolol (all the ones from N to Z on the alphabet)
Which drugs are alpha AND beta blockers?
Carvedilol and Labetalol (do not ened in “-olol”)
Antidote for acetaminophen…
N-acetylcysteine (replenishes glutathione)
Antidote for AChE inhibitors…
Atropine (agonist) followed by pralidoxine (removes AChE blockade)
Antidote for Amphetamines…
NH4Cl to acidify urine
Antidote for anticholinergics…
Physostigmine and control of hyperthermia
Antidote for benzodiazepines…
Flumazenil (GABA_A antagonist)
Antidote for beta-blockers…
Glucagon
Antidote for carbon monoxide…
Hyperbaric O2
Antidote for copper, arsenic or gold…
Penicillamine (chelator)
Antidote for cyanide…
Nitrite (oxidizes hemoglobin and prevents binding by cyanide) and thiosulfate
Antidote for methemoglobin or nitrite…
Methylene blue (turns methemoglobin back to hemoglobin)
Antidote for digitalis…
Anti-dig Fab fragments
Antidote for heparine…
Protamine sulfate
Antidote for Iron…
Deferoxamine or Deferasirox
Antidote for lead…
EDTA, dimercaprol, succiner, penicillamine
Antidote for mercury, arsenic or gold…
diMERcaprol, succiner
Antidote for methanol or ethylene glycol…
Fomepizole
Antidote for opioids…
Naloxone (mu receptor inhibitor)
Antidote for salicylates…
NaHCO3 to alk the urine
Antidote for TCAs…
NaHCO3 to alk the plasma
Antidote for tPA, streptokinase or urokinase…
Aminocaproic acid
Antidote for Warfarin…
Vitamin K
Antibiotics ending in -azole
Ergosterol synthesis inhibitors
Antibiotics ending in -bendazole
Anti helmintic or anti parasitic
Antibiotics ending in -cilin
Peptidoglycan synthesis inhibitor
Antibiotics ending in -cycline
Aminoacyl-tRNA binding to 30S inhibition
Antibiotics ending in -ivir
Neuroaminase inhibitors
Antibiotics ending in -navir
Protease inhibitors
Antibiotics ending in -ovir
DNA polymerase inhibitor
Antibiotics ending in -thromycin
Macrolides that block translocation on 50S
CNS drugs that end in -ane
Inhaled general anesthetic (ie. halothane)
CNS drugs that end in -azine
Typical anti-psychotics
CNS drugs that end in -barbital
Barbiturates
CNS drugs that end in -caine
Local anesthetic
CNS drugs that end in -etine
SSRI
CNS drugs that end in -ipramine
TCA
CNS drugs that end in -triptan
5-HT_{1B/1D} agonist (ie. sumatriptan)
CNS drugs that end in -triptyline
TCA
CNS drugs that end in -zepam
Benzodiazepine
CNS drugs that end in -zolam
Benzodiazepine
Autonomic drugs that end in -chol
Cholinergic agonist
Autonomic drugs that end in -curium or -curonium
Non-depolarizing muscular blocker derived from curare
Autonomic drugs that end in -olol
Beta blcoker
Autonomic drugs that end in -stigmine
AChE inhibitor
Autonomic drugs that end in -terol
Beta2 agonist
Autonomic drugs that end in -zosin
Alpha1 antagonist
Cardiovascular drugs that end in -afil
PDE-5 inhibitors
Cardiovascular drugs that end in -dipine
Dihydropyridine CCB (Ca+ channel blocker of vasculature)
Cardiovascular drugs that end in -pril
ACE inhibitor
Cardiovascular drugs that end in -sartan
Angiotensin II receptor blcoker
Cardiovascular drugs that end in -statin
HMG-CoA reductase inhibitor
Drugs ending in -dronate
Biphosphonate
Drugs ending in -glitazone
PPAR-gamma activator (insulin sensitizer)
Drugs ending in -prazole
Proton Pump Inhibitor
Drugs ending in -prost
Prostaglandin analog
Drugs ending in -tidine
H2 antagonist (Cimitedine)
Drugs ending in -tropin
Pituitary hormone
Drugs ending in -ximab
These are chimeric monoclonal antibodies
Drugs ending in -zumab
These are humanized monoclonal antibodies
Which drugs can cause gynecomastia?
Spironalactone Marijuana (dope) Digitalis Estrogen Cimetadine Alcohol Heroin Dopamine D2 antagonist Ketoconazole [Some dope drugs easily cause awkward hairy DD knocker.]