firstaid - pharm(1) Flashcards
Cholinomimetics (direct)
Bethanechol
Carbachol
Pilocarpine
Methacholine
Bethanechol
activates bowel & bladder
postoperative ileus/neurogenic ileus, urinary retention treatment
Carbachol
carbon copy of Ach
glaucoma, relief of intraocular pressure
pupillary contraction
Pilocarpine
Stimulates sweat, tears, saliva
Open and close angle glaucoma
Resistant to acetylcholinesterase (AChE)
Methacholine
challenge test for ASTHMA
stimulates MUSCARINIC receptors in airway
Cholinomimetics (indirect) - ANTIcholinesterase
Neostigmine Pyridostigmine Edrophonium Physostigmine Donepezil
Neostigmine
Myasthenia gravis
postoperative/neurogenic ileus
urinary retention
Pyridostigmine
Myasthenia gravis (long acting) does NOT penetrate CNS
Edrophonium
Myasthenia gravis (diagnosis) -- SHORT acting Symptoms improve (proximal weakness - problems getting up from a chair, walking up stairs, eye drooping)
Physostigmine
Treats anticholinergic toxicity (reverse atropine toxicity) - crosses CNS
Donepezil
Alzheimer’s disease
Helps symptoms but does not cure disease
Side effects of ALL cholinomimetics
exacerbation of COPD, asthma, peptic ulcers
Cholinesterase inhibitor poisoning
too much acetylcholinesterase inhibitors
organophosphates poisoning (insecticides)
DUMBBELSS diarrhea urination miosis bronchospasm bradycardia excitation of skeletal muscle/CNS lacrimation sweating salivation
Reveral of cholinesterase inhibitor poisoning
ATROPINE + pralidoxime
Reversal of atropine poisoning
atropine is muscarinic antagonist - decreases actions of Ach
Physostigmine (cholinesterase inhibitor to INCREASE Ach)
Muscarinic antagonists
Benztropine Scopolamine Ipratropium Oxybutynin Glycopyrrolate
Atropine
Mydriasis (risk of acute angle closure glaucoma)
Cycloplegia (loss of accomodation)
Benztropine
treats Parkinson’s disease
Scopolamine
Motion sickness
muscarinic cholinergic ANTAGONIST
Ipratropium mechanism & uses
Asthma & COPD
muscarinic cholinergic receptor ANATAGONIST
Blocks action of Ach on muscarinic receptors (Ach released when vagal nerve stimulated –> parasympathetics –> bronchoconstriction)
Ipratropium is beta2 agonist – bronchodilation
Oxybutynin
anticholinergic
decrease urgency (cystitis) decrease bladder spasms due to antimuscarinic action to smooth muscle cells
Glycopyrrolate
decrease mucus secretion in airway
decrease drooling
decrease gastric secretion (peptic ulcer)
Atropine: actions
muscarinic antagonist
blocks DUMBBeLLS
increase pupil dilation, cycloplegia decrease secretions decrease acid secretion decrease motility decrease urgency in cystitis
skeletal m. and CNS excitation mediated by nicotinic receptors (not affected by atropine)
Atropine toxicity: symptoms
increase body temperature (decrease sweating)
dry, flushed skin (peripheral vasodilation bc of no sweating)
cycloplegia (loss of accomodation)
acute angle closure glaucoma (in elderly)
urinary retention (old men w/ BPH)
hyperthermia (infants)
“hot, dry, red, blind, mad”
Sympathomimetics (direct)
Epinephrine Norepinephrine Isoproterenol Dopamine Dobutamine Phenylephrine Albuterol, Salmeterol, Terbutaline Ritodrine
Epinephrine
alpha 1&2, beta 1&2
Indication:
anaphylaxis, glaucoma (open)
asthma
hypotension
Norepinephrine
alpha 1&2, beta 1
NO beta 2
Indication:
hypotension
(but DECREASE renal perfusion - bad!)
Isoproterenol
beta 1&2
Indication:
torsade de pointes
bradyarrhythmias (but worsens ischemia)
Dopamine
high dose - alpha 1&2
medium dose - beta 1&2
low dose - D1
Indications:
a) SHOCK (renal perfusion - raises BP)
b) Heart failure
c) Ionotropic (heart contraction) & chronotropic (heart rate)
Dobutamine
beta 1 agonist MAINLY
some alpha 1&2 (inotropic & chronotropic)
Indication:
HEART FAILURE
Phenylephrine
alpha 1&2
Actions:
Hypotension (vasoconstrictor)
Mydriasis (ocular procedures)
Decongestant (rhinitis)
Albuterol
Salmeterol
Terbutaline
beta 2 agonist MAINLY
some beta 1
metaproterenol & albuterol = acute asthma
salmeterol = long term asthma/COPD
terbutaline = prevent premature uterine contractions
Ritodrine
beta 2 agonist
reduce premature uterine contractions
Sympathomimetics (indirect)
Increase catecholamine release or decrease reuptake
Amphetamine
Ephedrine
Cocaine
Amphetamine
release stored catecholamines
narcolepsy
obesity
ADHD
Ephedrine
releases stored catecholamines
nasal decongestant
urinary incontinence
hypotension
Cocaine
catecholamine reuptake inhibitor
vasoconstriction
local anesthesia
*never give beta blockers if cocaine intoxication suspected (unopposed alpha 1 activation –> severe HTN)
Clonidine
alpha-methyldopa
Sympathoplegics
alpha-2 agonist
decrease sympathetic outflow
HTN (good for renal failure pts. bc it doesn’t compromise blood flow to kidneys)
alpha blockers (nonselective)
phenoxybenzamine
phentolamine
phenoxybenzamine (irreversible)
nonselective alpha adrenergic ANTAGONIST
pheochromocytoma
toxicity: orthostatic hypotension, reflex tachycardia
phentolamine (reversible)
treats patients on MAO inhibitors that eat tyramine-containing foods
alpha 1 selective inhibitors
“-osin” (prazosin)
HTN urinary retention (BPH)
alpha 2 selective inhibtors
mirtazapine (increase outflow of sympathetics)
Rx for: depression
Beta blockers (selectivity)
“-olol”
A-M are beta1 selective antagonists
N-Z are nonselective beta antagonists
beta 1 selective prefered for patients w/ comorbid PULMONARY disease (beta 2 antagonists causes bronchoconstriction)
Beta blocker: angina pectoris
Decrease HR and contractility –> decrease O2 consumption
Beta blocker: MI
decrease mortality
Beta blocker: SVT (metoprolol, esmolol)
Metoprolol, Esmolol
Decrease AV conduction velocity (class II antiarrhythmic)
Beta blocker: HTN
Decrease CO
Decrease renin secretion (B1 receptor block on JGA cells)
Beta blocker: CHF
Slows progression of chronic failure
Beta blocker: Glaucoma
Timolol
Decrease secretion of aqueous humor
Nonselective alpha&beta antagonists
Carvedilol
Labetalol
Beta blockers w/ PARTIAL beta-agonistic activity (intrinsic sympathomimetic activity)
Pindolol
Acebutolol
Toxicity of B-blockers
a) Impotence (smooth muscle relaxation)
b) Exacerbation of asthma (B2 bronchodilation inhibited)
c) Bradycardia, AV block, CHF
d) Seizures, sedation, sleep alterations
B-blockers used w/ diabetics
Blunt symptoms of hypoglycemia – use w/ caution!
P450 inducers
Modafinil Barbiturates St. John's wort Phenytoin Rifampin Griseofulvin Carbamazepine Chronic alcohol use
P450 inhibitors
Quinidine Ciprofloxacin Isoniazid Grapefruit juice Acute alcohol use Erythromycin Indinavir Cimetidine Sulfonamides Ketoconazole Amiodarone Macrolides (some) Gemfibrozil
Sulfa drugs (8)
Probenecid Furosemide Acetazolamide Celecoxib Thiazides Sulfonamide antibiotics Sulfasalazine Sulfonylureas
Sulfa allergies: Stevens-Johnson UTI pruritic rash, urticaria (hives) hemolytic anemia, thrombocytopenia, agranulocytosis
-navir
protease inhibitor
Saquinavir
-triptan
5-HT 1B/1D agonist
Sumatriptan
-ane
Inhalational general anesthetic
Halothane
-caine
Local anesthetic
Lidocaine
-operidol
butyrphenone (neuroleptic)
Haloperidol
-azine
Phenothiazine (neuroleptic, antiemetic)
Chlorpromazine
-barbital
Barbituate
Phenobarbital
-zolam
BENZO
Alprazolam
-azepam
BENZO
Diazepam
-etine
SSRI
Fluoxetine – side effect: sexual dysfunction
-ipramine
TCA
Imipramine
-triptyline
TCA
Amitriptyline
-olol
b-antagonist
Propranolol
-terol
b2 agonist
Albuterol
-zosin
a1 antagonist
Prazosin
-oxin
Cardiac glycoside (inotropic)
Digoxin
-pril
Captopril
-afil
Erectile dysfunction
Sildenafil
-tropin
Pituitary hormone
Somatotropin
-tidine
H2 antagnoist
Cimetidine
Antidote: acetaminophen
N-acetylcysteine (replenishes glutathione)
Antidote: salicylates
NaHCO3 (alkalinize urine)
Dialysis
Antidote: amphetamines (basic)
NH4Cl (acidify urine)
Antidote: Acetylcholinesterase inhibitors, organophosphates
TOO MUCH ACH!
Atropine
Pralidoxime
Antidote: Antimuscarinic Anticholinergic agents (eg. Atropine toxicity)
Physostigmine salicylate
Control hyperthermia
Antidote: B-blockers
Glucagon
Antidote: Digitalis
Normalize K+
Lidocaine
Anti-dig Fab fragments
Mg2+
Antidote: Iron
DeFEroxamine
DeFErasirox
Antidote: Lead
CaEDTA
Dimercaprol
Succimer
Penicillamine
Antidote: Mercury, arsenic, gold
Dimercaprol
Succimer
Antidote: Copper, arsenic, gold
Penicillamine
Antidote: Cyanide
Nitrite + thiosulfate
Hydroxocobalamin
Antidote: Methemoglobin
Methylene blue
Vitamin C
Antidote: Carbon monoxide
100% O2
Hyperbaric O2
Antidote: Methanol, ethylene glycol (antifreeze)
Fomepizole > ethanol
Dialysis
Antidote: Opioids
Naloxone
Naltrexone
Antidote: Benzodiazepines
Flumazenil
Antidote: TCAs
NaHCO3 (plasma alkalinization)
Antidote: Heparin
Protamine
Antidote: Warfarin
Vitamin K
Fresh frozen plasma
Antidote: tPA, streptokinase, urokinase
Aminocaproic acid
Antidote: Theophylline
B-blocker
G-protein linked 2nd messengers (5)
Sympathethic Parasympathetic Dopamine Histamine Vasopressin
Sympathethic
a1 - q
a2 - i
b1 - s
b2 - s
a1 receptor (3)
a) Increase vascular smooth muscle contraction
b) Increase pupillary dilatory muscle contraction (mydriasis – dilate)
c) Increase intestinal & bladder sphincter muscle contraction
a2 receptor (4)
a) DECREASE sympathetic outflow
b) DECREASE insulin release
c) DECREASE lipolysis
d) Increase platelet aggregation*
b1 receptor (4)
a) Increase HR
b) Increase contractility
c) Increase renin release
d) Increase lipolysis
b2 receptor (7)
a) Vasodilation
b) Bronchodilation
c) Increase HR, contractility; Increase lipolysis (similar to b1 receptor actions)
d) INCREASE insulin release
e) DECREASE uterine tone (delay childbirth) - tocolysis
f) Ciliary muscle relaxation
g) Increase aqueous humor production
Parasympathetic
M1 - q
M2 - i
M3 - q
M1 receptor
CNS
Enteric nervous system
M2 receptor (2)
Decrease HR
Decrease contractility of atria
Atropine inhibits M2 –> given for pts. w/ bradycardia
M3 receptor (6)
a) Increase exocrine gland secretions (lacrimal, gastric acid)
b) Increase gut peristalsis
c) Increase bladder contraction
d) Bronchoconstriction
e) Increase pupillary sphincter muscle contraction (miosis)
f) Ciliary muscular contraction (accomodation)
Dopamine
D1 - s
D2 - i
D1 receptor
Relaxes renal vascular smooth muscle (increase renal blood flow)
D2 receptor
Modulates transmitter release (esp in BRAIN)
Histamine
H1 - q
H2 - s
H1 receptor
a) Increase nasal and bronchial mucus production
b) Contraction of bronchioles
c) Pruritus
d) Pain
H2 receptor
Increase gastric acid secretion
Vasopressin
V1 - q
V2 - s
V1 receptor
Increase vascular smooth muscle contraction
V2 receptor
Increase H2O permeability & reabsorption in collecting tubules of kidney
Gq receptors
H1, a1, V1, M1, M3
“HAVe 1 M&M”
Function of Gq
Receptor –> Gq –> phospholipase C –> Lipids cleaved to PIP2; PIP2 cleaved to DAG and IP3 via phospholipase C
DAG –> protein kinase C –> phosphorylation of downstream messengers
IP3 –> Increase intracellular Ca2+ –> smooth muscle contraction
Qs receptors
b1, b2, D1, H2, V2
Qi receptors
M2, a2, D2
“MAD 2’s”
Function of Gs and Gi
Receptor –> Gs or Gi –> Adenyl cyclase –> ATP to cAMP –> protein kinase A
Protein kinase A –>
a) Increase intracellular Ca2+ (heart)
b) Myosin light chain kinase (smooth muscle)
Glaucoma drugs
Decrease intraocular pressure via decrease amount of aqueous humor (increase drainage, inhibit synthesis or secretion)
Types of glaucoma drugs (5)
1) a-agonist
2) b-blockers
3) diuretics
4) cholinomimetics
5) prostaglandin
Glaucoma drugs: a-agonists
EPI: decrease aqueous humor synthesis via VASOCONSTRICTION
Brimonidine (a2): decrease aqueous humor synthesis
Side effects of EPI and Brimonidine for glaucoma treatment
Mydriasis (dilated pupils)
Blurry vision, ocular hyperemia, foreign body sensation, ocular allergic rxns, ocular pruritus
What type of glaucoma should you never use EPI or Brimonidine for?
Closed-angle glaucoma
Glaucoma drugs: b-blockers
Timolol
Betaxolol
Carteolol
No pupillary or vision changes - no side effects!!
Glaucoma drugs: diuretics
Acetazolamide
Decrease aqueous humor synthesis via inhibition of carbonic anhydrase
No pupillary or vision changes - no side effects!!
Glaucoma drugs: cholinomimetics
Direct: pilocarpine, carbachol
Indirect: physostigmine, echotiophate
ALL increase drainage of aqueous fluid
Pilocarpine Carbachol Physostigmine Echothiophate (MOA)
Increase outflow of aqueous humor via contraction of ciliary m. –> opens trabecular meshwork
Use Pilocarpine in EMERGENCIES - very effective at opening meshwork into canal of Schlemm
Pilocarpine Carbachol Physostigmine Echothiophate (side effects)
Miosis
Cyclospasm (contraction of ciliary m.)
Glaucoma drugs: prostaglandin
Latanoprost (PGF2a)
Increase outflow of aqueous humor
Latanoprost (side effect)
Darkens color of iris (browning)
Opioid analgesic
Morphine Fentanyl Codeine Heroin Methadone Meperidine Dextromethorphan Diphenoxylate