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firstaid - pharm(1) Flashcards

1
Q

Cholinomimetics (direct)

A

Bethanechol
Carbachol
Pilocarpine
Methacholine

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2
Q

Bethanechol

A

activates bowel & bladder

postoperative ileus/neurogenic ileus, urinary retention treatment

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3
Q

Carbachol

A

carbon copy of Ach
glaucoma, relief of intraocular pressure
pupillary contraction

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4
Q

Pilocarpine

A

Stimulates sweat, tears, saliva
Open and close angle glaucoma

Resistant to acetylcholinesterase (AChE)

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5
Q

Methacholine

A

challenge test for ASTHMA

stimulates MUSCARINIC receptors in airway

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6
Q

Cholinomimetics (indirect) - ANTIcholinesterase

A 
Neostigmine
Pyridostigmine
Edrophonium
Physostigmine
Donepezil
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7
Q

Neostigmine

A

Myasthenia gravis
postoperative/neurogenic ileus
urinary retention

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8
Q

Pyridostigmine

A 
Myasthenia gravis (long acting)
does NOT penetrate CNS
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9
Q

Edrophonium

A 
Myasthenia gravis (diagnosis) -- SHORT acting
Symptoms improve (proximal weakness - problems getting up from a chair, walking up stairs, eye drooping)
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10
Q

Physostigmine

A

Treats anticholinergic toxicity (reverse atropine toxicity) - crosses CNS

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11
Q

Donepezil

A

Alzheimer’s disease

Helps symptoms but does not cure disease

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12
Q

Side effects of ALL cholinomimetics

A

exacerbation of COPD, asthma, peptic ulcers

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13
Q

Cholinesterase inhibitor poisoning

too much acetylcholinesterase inhibitors

A

organophosphates poisoning (insecticides)

DUMBBELSS
diarrhea
urination
miosis
bronchospasm
bradycardia
excitation of skeletal muscle/CNS
lacrimation
sweating
salivation
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14
Q

Reveral of cholinesterase inhibitor poisoning

A

ATROPINE + pralidoxime

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15
Q

Reversal of atropine poisoning

atropine is muscarinic antagonist - decreases actions of Ach

A

Physostigmine (cholinesterase inhibitor to INCREASE Ach)

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16
Q

Muscarinic antagonists

A 
Benztropine
Scopolamine
Ipratropium
Oxybutynin
Glycopyrrolate
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17
Q

Atropine

A

Mydriasis (risk of acute angle closure glaucoma)

Cycloplegia (loss of accomodation)

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18
Q

Benztropine

A

treats Parkinson’s disease

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19
Q

Scopolamine

A

Motion sickness

muscarinic cholinergic ANTAGONIST

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20
Q

Ipratropium mechanism & uses

A

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

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21
Q

Oxybutynin

A

anticholinergic

decrease urgency (cystitis)
decrease bladder spasms due to antimuscarinic action to smooth muscle cells
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22
Q

Glycopyrrolate

A

decrease mucus secretion in airway
decrease drooling
decrease gastric secretion (peptic ulcer)

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23
Q

Atropine: actions

A

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)

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24
Q

Atropine toxicity: symptoms

A

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”

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25
Sympathomimetics (direct)
``` Epinephrine Norepinephrine Isoproterenol Dopamine Dobutamine Phenylephrine Albuterol, Salmeterol, Terbutaline Ritodrine ```
26
Epinephrine
alpha 1&2, beta 1&2 Indication: anaphylaxis, glaucoma (open) asthma hypotension
27
Norepinephrine
alpha 1&2, beta 1 NO beta 2 Indication: hypotension (but DECREASE renal perfusion - bad!)
28
Isoproterenol
beta 1&2 Indication: torsade de pointes bradyarrhythmias (but worsens ischemia)
29
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)
30
Dobutamine
beta 1 agonist MAINLY some alpha 1&2 (inotropic & chronotropic) Indication: HEART FAILURE
31
Phenylephrine
alpha 1&2 Actions: Hypotension (vasoconstrictor) Mydriasis (ocular procedures) Decongestant (rhinitis)
32
Albuterol Salmeterol Terbutaline
beta 2 agonist MAINLY some beta 1 metaproterenol & albuterol = acute asthma salmeterol = long term asthma/COPD terbutaline = prevent premature uterine contractions
33
Ritodrine
beta 2 agonist | reduce premature uterine contractions
34
Sympathomimetics (indirect)
Increase catecholamine release or decrease reuptake Amphetamine Ephedrine Cocaine
35
Amphetamine
release stored catecholamines narcolepsy obesity ADHD
36
Ephedrine
releases stored catecholamines nasal decongestant urinary incontinence hypotension
37
Cocaine
catecholamine reuptake inhibitor vasoconstriction local anesthesia *never give beta blockers if cocaine intoxication suspected (unopposed alpha 1 activation --> severe HTN)
38
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)
39
alpha blockers (nonselective)
phenoxybenzamine | phentolamine
40
phenoxybenzamine (irreversible)
nonselective alpha adrenergic ANTAGONIST pheochromocytoma toxicity: orthostatic hypotension, reflex tachycardia
41
phentolamine (reversible)
treats patients on MAO inhibitors that eat tyramine-containing foods
42
alpha 1 selective inhibitors
"-osin" (prazosin) ``` HTN urinary retention (BPH) ```
43
alpha 2 selective inhibtors
mirtazapine (increase outflow of sympathetics) Rx for: depression
44
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)
45
Beta blocker: angina pectoris
Decrease HR and contractility --> decrease O2 consumption
46
Beta blocker: MI
decrease mortality
47
Beta blocker: SVT (metoprolol, esmolol)
Metoprolol, Esmolol Decrease AV conduction velocity (class II antiarrhythmic)
48
Beta blocker: HTN
Decrease CO Decrease renin secretion (B1 receptor block on JGA cells)
49
Beta blocker: CHF
Slows progression of chronic failure
50
Beta blocker: Glaucoma
Timolol Decrease secretion of aqueous humor
51
Nonselective alpha&beta antagonists
Carvedilol | Labetalol
52
Beta blockers w/ PARTIAL beta-agonistic activity (intrinsic sympathomimetic activity)
Pindolol | Acebutolol
53
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
54
B-blockers used w/ diabetics
Blunt symptoms of hypoglycemia -- use w/ caution!
55
P450 inducers
``` Modafinil Barbiturates St. John's wort Phenytoin Rifampin Griseofulvin Carbamazepine Chronic alcohol use ```
56
P450 inhibitors
``` Quinidine Ciprofloxacin Isoniazid Grapefruit juice Acute alcohol use Erythromycin Indinavir Cimetidine Sulfonamides Ketoconazole Amiodarone Macrolides (some) Gemfibrozil ```
57
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 ```
58
-navir
protease inhibitor Saquinavir
59
-triptan
5-HT 1B/1D agonist Sumatriptan
60
-ane
Inhalational general anesthetic Halothane
61
-caine
Local anesthetic Lidocaine
62
-operidol
butyrphenone (neuroleptic) Haloperidol
63
-azine
Phenothiazine (neuroleptic, antiemetic) Chlorpromazine
64
-barbital
Barbituate Phenobarbital
65
-zolam
BENZO Alprazolam
66
-azepam
BENZO Diazepam
67
-etine
SSRI Fluoxetine -- side effect: sexual dysfunction
68
-ipramine
TCA Imipramine
69
-triptyline
TCA Amitriptyline
70
-olol
b-antagonist Propranolol
71
-terol
b2 agonist Albuterol
72
-zosin
a1 antagonist Prazosin
73
-oxin
Cardiac glycoside (inotropic) Digoxin
74
-pril
Captopril
75
-afil
Erectile dysfunction Sildenafil
76
-tropin
Pituitary hormone Somatotropin
77
-tidine
H2 antagnoist Cimetidine
78
Antidote: acetaminophen
N-acetylcysteine (replenishes glutathione)
79
Antidote: salicylates
NaHCO3 (alkalinize urine) | Dialysis
80
Antidote: amphetamines (basic)
NH4Cl (acidify urine)
81
Antidote: Acetylcholinesterase inhibitors, organophosphates | TOO MUCH ACH!
Atropine | Pralidoxime
82
``` Antidote: Antimuscarinic Anticholinergic agents (eg. Atropine toxicity) ```
Physostigmine salicylate | Control hyperthermia
83
Antidote: B-blockers
Glucagon
84
Antidote: Digitalis
Normalize K+ Lidocaine Anti-dig Fab fragments Mg2+
85
Antidote: Iron
DeFEroxamine | DeFErasirox
86
Antidote: Lead
CaEDTA Dimercaprol Succimer Penicillamine
87
Antidote: Mercury, arsenic, gold
Dimercaprol | Succimer
88
Antidote: Copper, arsenic, gold
Penicillamine
89
Antidote: Cyanide
Nitrite + thiosulfate | Hydroxocobalamin
90
Antidote: Methemoglobin
Methylene blue | Vitamin C
91
Antidote: Carbon monoxide
100% O2 | Hyperbaric O2
92
Antidote: Methanol, ethylene glycol (antifreeze)
Fomepizole > ethanol | Dialysis
93
Antidote: Opioids
Naloxone | Naltrexone
94
Antidote: Benzodiazepines
Flumazenil
95
Antidote: TCAs
NaHCO3 (plasma alkalinization)
96
Antidote: Heparin
Protamine
97
Antidote: Warfarin
Vitamin K | Fresh frozen plasma
98
Antidote: tPA, streptokinase, urokinase
Aminocaproic acid
99
Antidote: Theophylline
B-blocker
100
G-protein linked 2nd messengers (5)
``` Sympathethic Parasympathetic Dopamine Histamine Vasopressin ```
101
Sympathethic
a1 - q a2 - i b1 - s b2 - s
102
a1 receptor (3)
a) Increase vascular smooth muscle contraction b) Increase pupillary dilatory muscle contraction (mydriasis -- dilate) c) Increase intestinal & bladder sphincter muscle contraction
103
a2 receptor (4)
a) DECREASE sympathetic outflow b) DECREASE insulin release c) DECREASE lipolysis d) Increase platelet aggregation*
104
b1 receptor (4)
a) Increase HR b) Increase contractility c) Increase renin release d) Increase lipolysis
105
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
106
Parasympathetic
M1 - q M2 - i M3 - q
107
M1 receptor
CNS | Enteric nervous system
108
M2 receptor (2)
Decrease HR Decrease contractility of atria Atropine inhibits M2 --> given for pts. w/ bradycardia
109
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)
110
Dopamine
D1 - s | D2 - i
111
D1 receptor
Relaxes renal vascular smooth muscle (increase renal blood flow)
112
D2 receptor
Modulates transmitter release (esp in BRAIN)
113
Histamine
H1 - q | H2 - s
114
H1 receptor
a) Increase nasal and bronchial mucus production b) Contraction of bronchioles c) Pruritus d) Pain
115
H2 receptor
Increase gastric acid secretion
116
Vasopressin
V1 - q | V2 - s
117
V1 receptor
Increase vascular smooth muscle contraction
118
V2 receptor
Increase H2O permeability & reabsorption in collecting tubules of kidney
119
Gq receptors
H1, a1, V1, M1, M3 "HAVe 1 M&M"
120
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
121
Qs receptors
b1, b2, D1, H2, V2
122
Qi receptors
M2, a2, D2 "MAD 2's"
123
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)
124
Glaucoma drugs
Decrease intraocular pressure via decrease amount of aqueous humor (increase drainage, inhibit synthesis or secretion)
125
Types of glaucoma drugs (5)
1) a-agonist 2) b-blockers 3) diuretics 4) cholinomimetics 5) prostaglandin
126
Glaucoma drugs: a-agonists
EPI: decrease aqueous humor synthesis via VASOCONSTRICTION Brimonidine (a2): decrease aqueous humor synthesis
127
Side effects of EPI and Brimonidine for glaucoma treatment
Mydriasis (dilated pupils) Blurry vision, ocular hyperemia, foreign body sensation, ocular allergic rxns, ocular pruritus
128
What type of glaucoma should you never use EPI or Brimonidine for?
Closed-angle glaucoma
129
Glaucoma drugs: b-blockers
Timolol Betaxolol Carteolol No pupillary or vision changes - no side effects!!
130
Glaucoma drugs: diuretics
Acetazolamide Decrease aqueous humor synthesis via inhibition of carbonic anhydrase No pupillary or vision changes - no side effects!!
131
Glaucoma drugs: cholinomimetics
Direct: pilocarpine, carbachol Indirect: physostigmine, echotiophate ALL increase drainage of aqueous fluid
132
``` 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
133
``` Pilocarpine Carbachol Physostigmine Echothiophate (side effects) ```
Miosis Cyclospasm (contraction of ciliary m.)
134
Glaucoma drugs: prostaglandin
Latanoprost (PGF2a) Increase outflow of aqueous humor
135
Latanoprost (side effect)
Darkens color of iris (browning)
136
Opioid analgesic
``` Morphine Fentanyl Codeine Heroin Methadone Meperidine Dextromethorphan Diphenoxylate ```
137
Opioid: MOA
Agonist at opioid receptors (mu = morphine, delta = enkephalin, kappa = dynorphin) --> modulates synaptic transmission Open K+ channels --> close Ca2+ channels --> DECREASE synaptic transmission
138
Opioids inhibit release of what substances?
``` ACh NE 5-HT Glutamate substance P ```
139
Opioid: Indications
``` Pain Cough suppression Diarrhea Acute pulmonary edema Maintennance programs for addicts ```
140
What opioid is used for cough suppression?
Dextromethorphan
141
What opioid is used for diarrhea?
Loperamide | Diphenoxylate
142
What opioid is used for maintennace programs for addicts?
Methadone
143
Opioid: Toxicity
``` Addiction Respiratory depression Constipation Miosis (pinpoint pupils) CNS depression (additive w/ other drugs) ```
144
How do you treat opioid overdose?
Naloxone Naltrexone Both are opioid receptor antagonists
145
Butorphanol: MOA
Mu opioid receptor PARTIAL agonist Kappa opoid receptor agonist Analgesia
146
Butorphanol: Indications
Severe pain (migraine, labor) Causes less respiratory depression than full opioid agonists
147
Butorphanol: Toxicity
Opioid withdrawal symptoms if patient is also taking full opioid agonist (competition for opioid receptors) Overdose NOT easily reversed w/ Naloxone
148
Tramadol: MOA
Very weak opioid agonist Inhibits serotonin and NE reuptake (works on multiple neurotransmitters)
149
Tramadol: Indications
Chronic pain
150
Tramadol: Toxicity
Similar to opioids Decreases seizure threshold*
151
Phenytoin: MOA
Blocks Na2+ channels | Inhibit glutamate release (no excitation)
152
Phenytoin: Indications
Tonic-clonic seizures Class IB antiarrhythmic
153
Phenytoin: Toxicity (8)
1. Nystagmus, diplopia, ataxia, sedation 2. Gingival hyperplasia (children) 3. SLE-like syndrome 4. Induction of cytP450 5. Megaloblastic anemia (decrease folate absorption) 6. Tetratogenesis (fetal hydantoin syndrome) 7. Stevens-Johnson 8. Osteopenia
154
Barbituates (4)
Phenobarbital Pentobarbital Thiopental Secobarbital
155
Barbituates: MOA
Increase DURATION of Cl- channels opening --> DECREASE neuron firing --> potentiates GABA action
156
Barbituates: Indications
Sedative for: | Anxiety, Seizures, Insomnia, Induction of anesthesia
157
What barbituate is used for induction of anesthesia?
Thiopental
158
When is barbituates contraindicated?
Porphyria
159
Barbituates: Toxicity
Respiratory and cardiovascular depression (can be fatal!!) CNS depression (exacerbated w/ ethanol use) Drug interactions (p450 inducer)
160
Overdose of barbituates: treatment?
Supportive - assist respiration & maintain BP
161
Benzodiazepines (8)
``` Diazepam Lorazepam Triazolam Temazepam Oxazepam Midazolam Chlordiazepoxide Alprazolam ```
162
Benzodiazepines: MOA
Increase FREQUENCY of Cl- channel opening --> potentiates GABA action Long half lives (except Triazolam, Oxazepam, Midazolam = short acting)
163
Benzodiazepines: Indications
``` Anxiety Spasticity Status epilepticus (lorazepam, diazepam) Detoxification (alcohol withdrawal-DTs) Sleep walking General anesthetic (amnesia, muscle relaxation) Hypnotic (insomnia) ```
164
Which benzos are used especially for status epilepticus?
Lorazepam | Diazepam
165
Benzodiazepines: Toxicity
Dependence Additive CNS depression w/ alcohol LESS risk of respiratory depression & coma than barbituates
166
Which benzos are short acting (therefore have high addictive potential)?
Triazolam Oxazepam Midazolam
167
Treatment for benzodiazepines overdose:
Flumazenil (competitive antagonist at GABA benzodiazepine receptor)
168
Non-benzodiazepine hypnotics
Zolpidem (Ambien) Zaleplon Eszopiclone
169
Zolpidem: MOA
Act via BZ1 subtype of GABA receptor
170
Zolpidem: Indications
Insomnia
171
Zolpidem: Toxicity
Ataxia, headaches, confusion Short duration --> rapid metabolism by liver enzymes Cause only modest day-after psychomotor depression; few amnestic effects LOWER dependence risk than benzodiazepines
172
Treatment for Zolpidem toxicity
Flumazenil
173
Anesthetics: general principles
CNS drugs -- must be LIPID SOLUBLE (cross BBB) or be actively transported DECREASE solubility in BLOOD --> rapid induction/recovery INCREASE solubility in LIPIDS --> increase potency (1/MAC) -- smaller MAC equals greater potency (MAC = minimal alveolar concentration at which 50% of pts. anesthetized)
174
Halothane vs. N2O: potency and solubility profile
N2O has DECREASE blood and lipid solubility --> fast induction - low potency Halothane has INCREASE blood and lipid solubility --> slow induction - high potency
175
Inhaled anesthetics (6)
Halothane "-flurane": Enflurane, Isoflurane, Sevoflurane, Methoxyflurane Nitrous oxide
176
Halothane Enflurane/Isoflurane Nitrous oxide (Indications)
MI depression Respiratory depression Increase cerebral blood flow (decrease cerebral metabolic demand)
177
Halothane: toxicity
Hepatotoxic
178
Methoxyflurane: toxicity
Nephrotoxic
179
Enflurane: toxicity
Pro-convulsant
180
All inhaled anesthetics (except nitrous oxide) have increased risk of:
Malignant hyperthermia
181
Nitrous oxide: toxicity
Expansion of trapped gas in body cavity
182
IV anesthetics (5)
Barbituates (increase duration of Cl- channels opening) Benzodiazepines (increase frequency of Cl- channels opening) Ketamine Opioids Propofol
183
IV anesthetic: Thiopental
high potency - high lipid solubility RAPID entry in brain *Induction of anesthesia, short surgical procedures effect terminated by RAPID REDISTRIBUTION into tissue (skeletal muscle) & fat decrease cerebral blood flow (sedation/sleep effect) Postoperative nausea
184
IV anesthethic: Midazolam
Endoscopy | Used w/ gaseous anesthetics & narcotics
185
Midazolam: toxicity
Severe postoperative respiratory depression Decrease BP (treat w/ flumazenil) Amnesia
186
IV anesthetic: Ketamine
PCP analogs Block NMDA receptors Cardiovascular stimulant
187
Ketamine: toxicity
Hallucination, bad dreams Increase cerebral blood flow
188
IV anesthetic: Opioids
Morphine Fentanyl Used w/ other drugs during general anesthesia
189
IV anesthetic: Propofol
Sedation in ICU Rapid anesthesia induction in short procedures Less postoperative nausea than thiopental Potentiates GABA
190
Local anesthetics
Esters: Procaine, Cocaine, Tetracaine Amides: Lidocaine, Mepivacaine, Bupivacaine (AmIdes have 2 "I"s)
191
Local anesthetics: MOA
Block activated Na+ channels (effective in rapidly firing neurons) Given w/ vasoconstrictors (EPI) to enhance local action Decrease bleeding Increase anesthesia by decrease systemic concentration
192
Local anesthetics: Indications
Minor surgical procedures Spinal anesthesia Give amides if pt. is allergic to esters
193
Alkaline anesthetics in infected (acidic) tissue
Alkaline anesthetics are charged - can't penetrate membrane --> need more anesthetics
194
Order of nerve blockade
Small diameter fibers before large fibers Myelinated fibers before unmyelinated (SIZE matters the most!!)
195
Order of sensation loss
1. Pain 2. Temperature 3. Touch 4. Pressure
196
Local anesthetics: Toxicity
``` CNS excitation Cardiovascular toxicity (Bupivacaine) HTN Hypotension Arrhythmias (Cocaine) ```
197
Local anesthetics: cardiovascular toxicity
Bupivacaine
198
Local anesthetics: arrhythmias
Cocaine
199
Neuromuscular blocking drugs: general uses
Muscle paralysis (relaxer) in surgery Mechanical ventilation Selective for motor nicotinic receptor
200
Neuromuscular blocking: depolarizing
Succinylcholine Strong Ach receptor agonist -- SUSTAINED depolarization --> no repolarization --> no muscle contraction
201
Reversal of Succinylcholine blockade
Phase I: prolonged depolarization - no antidote (block potentiated by cholinesterase inhibitors) Phase II: repolarized but blocked; Ach receptors available but desensitized Antidote for phase II: cholinesterase inhibitor (Neostigmine) --> increase Ach available so that when receptors become available --> mm. contraction resumes
202
Complications of Succinylcholine
Hypercalcemia Hyperkalemia Malignant hyperthermia
203
Neuromuscular blocking: nondepolarizing
``` Tubocurarine Atracurium Mivacurium Pancuronium Vecuronium Rocuronium ``` Competitive antagonist - compete w/ Ach for receptors
204
Reversal of Tubocurarine, Atracurium, Vecuronium
Neostigmine (wake patients up from surgery) Edrophonium & other cholinesterase inhibitors
205
Dantrolene: MOA
Prevent release of Ca2+ from SR in skeletal muscle
206
Dantrolene: Indications
1) Malignant hyperthermia 2) Neuroleptic malignant syndrome (toxicity of antipsychotic drugs) Causes of malignant hyperthermia: a) Toxicity of inhalation anesthetics (Halothane, "-flurane"); N2O does not have this side effect b) Succinylcholine
207
Parkinsonism drugs: strategy
Parkinsonism: decrease dopamine; excess cholinergic activity Drug actions: 1) dopamine agonists 2) increase dopamine release 3) prevent dopamine breakdown 4) curb excess cholinergic activity
208
Bromocriptine (ergot) Pramipexole Ropinirole (non-ergot) -- preferred
Dopamine agonists
209
Amantadine (neuro & micro indications)
Increase dopamine release ANTIVIRAL against influenza A & Rubella
210
Amantadine: toxicity
Ataxia
211
L-dopa/Carbidopa
Converted to dopamine in CNS L-dopa crosses BBB --> converted to dopamine in CNS via dopa decarboxylase
212
Why is carbidopa given w/ L-dopa?
Limit peripheral side effects by inhibiting L-dopa conversion to dopamine peripherally --> increase amount of L-dopa available in the brain
213
Toxicity of L-dopa/Carbidopa
Arrhythmias from increased peripheral formation of catecholamines long term use: dyskinesia following administration
214
Selegiline: MOA
Selective MAO-B inhibitor MAO-B preferentially metabolizes dopamine over NE and 5-HT
215
Selegiline: Indications
Adjunctive agent to L-dopa in treatment of Parkinson's disease
216
Selegiline: Toxicity
Enhance adverse effects of L-dopa
217
Entacapone, Tolcapone
COMT inhibitors Inhibit L-dopa degradation --> increase dopamine availability
218
Benztropine
Antimuscarinic -- improves tremor & rigidity (little effect on bradykinesia)
219
Memantine: MOA
NMDAR antagonist Prevents excitotoxicity (mediated by Ca2+)
220
Memantine: Indications
Alzheimer's
221
Memantine: Toxicity
Hallucinations | Confusion
222
Donepezil Galantamine Rivastigmine (MOA)
Acetylcholinesterase inhibitors
223
Donepezil Galantamine Rivastigmine (Indications)
Alzheimer's
224
Donepezil Galantamine Rivastigmine (Toxicity)
Insomnia
225
Neurotransmitter changes in Huntington's disease
Decrease GABA Decrease ACh Increase Dopamine
226
Tetrabenazine Reserpine (MOA)
Inhibit VMAT --> limit dopamine vescile packaging & release Rx for Huntington's (too much dopamine)
227
Haloperidol
Dopamine receptor antagonist Rx for Huntington's (too much dopamine)
228
Sumatriptan: MOA
5-HT agonist Inhibits trigeminal nerve Prevents vasoactive peptide release Induces vasoconstriction Half life < 2hrs
229
Sumatriptan: Indications
Acute migraine | Cluster headache attacks
230
Sumatriptan: Toxicity
Coronary vasospasm | Mild tingling
231
When is sumatriptan contraindicated?
Patients w/ CAD or Prinzmetal's angina (due to coronary vasospasm side effect)
232
Rx: alcohol withdrawal
Benzodiazepines
233
Rx: anxiety
SSRIs SNRIs Buspirone
234
Rx: ADHD
Methylphenidate | Amphetamines
235
Rx: Bipolar disorder
Mood stabilizers: Lithium Valproic acid Carbamazepine Aytpical antipsychotics
236
Rx: Bulimia
SSRIs
237
Rx: Depression
SSRIs SNRIs TCAs Buspirone Mirtazapine (depression w/ insomnia)
238
Rx: OCD
SSRIs | Clomipramine
239
Rx: Panic disorder
SSRIs Venlafaxine Benzodiazepines
240
Rx: PTSD
SSRIs
241
Rx: Schizophrenia
Antipsychotics
242
Rx: Social phobias
SSRIs
243
Rx: Tourette's syndrome
Antipsychotics (Haloperidol, Risperidone)
244
CNS stimulants (3)
Methylphenidate Dextroamphetamine Methamphetamine
245
CNS stimulants: MOA
Increase catecholamines at synaptic cleft -- DOPAMINE & NE
246
CNS stimulants: Indications
ADHD Narcolepsy Appetite control
247
Typical Antipsychotics: "neuroleptics" (5)
Haloperidol ``` "-azines": Trifluoperazine Fluphenazine Thioridazine Chlorpromazine ```
248
Antipsychotics (typical): MOA
Block dopamine D2 receptors --> increase cAMP
249
Antipsychotics (typical): Indications
a) Schizophrenia (positive symptoms) b) Psychosis c) Acute mania d) Tourette's syndrome
250
Antipsychotics (typical): Toxicity
Highly soluble - stored in fat - very slow removal from body Extrapyramidal symptoms (dyskinesia) Endocrine: dopamine receptor antagonism --> hyperprolactinemia --> galactorrhea Blocking muscarinic: dry mouth, constipation Block a1 receptors: hypotension Block histamine receptors: sedation
251
High potency antipsychotics
Trifluoperazine Fluphenazine Haloperidol Extrapyramidal symptoms
252
Low potency antipsychotics
Chlorpromazine Thioridazine Non-neurologic side effects (anticholinergic, antihistamine, a1-blockade)
253
Chlorpromazine toxicity
Corneal deposits
254
Thioridazine toxicity
reTinal deposits
255
Haloperidol toxicity
Neuroleptic malignant syndrome Tardive dyskinesia (involuntary repetitive motions -- oral/facial motions) -- usually irreversible
256
Neuroleptic malignant syndrome (NMS)
Rigidity Myoglobinuria Autonomic instability Hyperpyrexia
257
Treatment for neuroleptic malignant syndrome
Dantrolene D2 agonists - Bromocriptine
258
Atypical antipsychotics (6)
``` Olanzapine Clozapine Quetiapine Risperidone Aripiprazole Ziprasidone ```
259
Atypical antipsychotics: Indications
a) Schizophrenia (positive & negative symptoms) b) Bipolar disorder c) OCD d) anxiety e) depression f) mania g) Tourette's syndrome
260
Atypical antipsychotics: Toxicity | esp. Olanzapine/clozapine; clozapine; Ziprasidone
LESS extrapyramidal and anticholinergic side effects than traditional antipsychotics Olanzapine/Clozapine: weight gain Clozapine: agranulocytosis (need WBC monitoring) Seizure Ziprasidone: prolonged QT interval
261
Lithium: Indications
Mood stabilizer: bipolar disorder Blocks relapse and acute manic events SIADH
262
What renal disorder is lithium used for?
SIADH
263
Lithium: Toxicity
``` Tremor Sedation Edema Heart block* Hypothyroidism ``` Polyuria (ADH antagonist --> nephrogenic DI) Teratogenesis (fetal cardiac defects = EBSTEIN's anomaly; malformation of great vessels)
264
Therapeutic index of Lithium
Narrow - requires constant monitoring of serum levels
265
Lithium excretion
Kidneys; most reabsorbed at PCT following Na+ reabsorption
266
Buspirone: MOA
Stimulates 5-HT receptors
267
Buspirone: Indications
Generalized anxiety disorder Takes 1-2 weeks to take effect No sedation/addiction/tolerance DOES NOT interact w/ alcohol (vs. barbituates, benzodiazepines)
268
Antidepressants (4)
1) SSRIs 2) SNRIs 3) TCAs 4) MAO inhibitors
269
SSRIs (4)
Fluoxetine Paroxetine Sertraline Citalopram
270
SSRIs: MOA
Serotonin-specifc reuptake inhibitors
271
SSRIs: Indications
``` Depression Generalized anxiety disorder Panic disorder OCD Bulimia Social phobias PTSD ```
272
SSRIs: Toxicity
FEWER toxicities than TCAs GI distress Sexual dysfunction (anorgasmia and decreased libido) Serotonin syndrome: (also seen w/ MAO inhibitors, SNRIs, TCAs -- all drugs that increase serotonin levels) 1) hyperthermia 2) myoclonus 3) cardiovascular collapse 4) flushing 5) diarrhea 6) seizures/confusion
273
Treatment of serotonin syndrome
Cyproheptadine (5-HT2 receptor antagonist) --> DECREASE serotonin levels
274
SNRIs (2)
Venlafaxine | Duloxetine
275
SNRIs: MOA
Inhibit serotonin and NE reuptake
276
SNRIs: Indications
DEPRESSION Venlafaxine: generalized anxiety & panic disorders Duloxetine: diabetic peripheral neuropathy (greater effect on NE)
277
SNRIs: Toxicity
Increase BP
278
TCAs
"-iptyline" -- Amitriptyline "-ipramine" -- Imipramine, Desipramine, Clomipramine Doxepin Amoxapine
279
TCAs: MOA
Blocks reuptake of NE and serotonin
280
TCAs: Indications (4)
Major depression Bedwetting (Imipramine) OCD (Clomipramine) Fibromyalgia
281
TCAs: Toxicity
a) Sedation b) a1 blockade --> postural hypotension c) atropine-like side effects (anticholinergic) -- tachycardia, urinary retention, dry mouth ``` Convulsions Coma Cardiotoxicity (arrhythmias) Respiratory depression Hyperpyrexia ```
282
Amitriptyline vs. Nortriptyline
Amitriptyline has MORE anticholinergic effects than Nortriptyline Use nortriptyline in elderly to decrease anticholinergic side effects (confusion/hallucinations)
283
Which TCA has least sedating effects and lower seizure threshold (easier for seizures to occur)?
Desipramine
284
What is given to treat arrhythmias caused by TCAs?
NaHCO3
285
Monoamine oxidase (MAO) inhibitors
Tranylcypromine Phenelzine Isocarboxazid Selegiline (selective MAO inhibitor)
286
MAO inhibitor: MOA
Nonselective MAO inhibition --> increase levels of amine neurotransmitters (NE, serotonin, dopamine)
287
MAO inhibitor: Indications
Atypical depression Anxiety Hypochondriasis (fear of having a malignant disease)
288
MAO inhibitor: Toxicity
Hypertensive crises (due to ingestion of tyramine via wine&cheese)
289
When is MAO inhibitor contraindicated?
``` Do not use MAO inhibitors w/: SSRIs TCAs St. John's Wort Meperidine Dextromethorphan (to prevent serotonin syndrome) ```
290
Atypical antidepressants (4)
Bupropion Mirtazapine Maprotiline Trazodone
291
Bupropion
Smoking cessation Increase NE and dopamine
292
Bupropion: toxicity
Tachycardia, insomnia (stimulant effects) Seizure in bulimic patients NO SEXUAL SIDE EFFECTS
293
Mirtazapine
a2-antagonist --> increase release of NE and serotonin Potent 5-HT2 and 5-HT3 receptor antagonist
294
Mirtazapine: toxicity
Sedation (desirable in depressed pts. w/ insomnia) Increased appetite, weight gain (desirable for elderly or anorexic pts.)
295
Maprotiline
Blocks NE reuptake
296
Maprotiline: toxicity
Sedation | Orthostatic hypotension
297
Trazodone
Inhibits serotonin reuptake Rx for insomnia -- higher doses for antidepressant effects
298
Trazodone: toxicity
Priapism (sustained erection; penis can't relax) | Postural hypotension
299
Drug rxn: coronary vasospasm
Cocaine Sumatriptan Ergot alkaloids
300
Drug rxn: cutaneous flushing
Vancomycin Adenosine Niacin Ca2+ channel blockers
301
Drug rxn: dilated cardiomyopathy
Doxorubicin (Adriamycin) | Daunorubicin
302
Drug rxn: Torsades de pointes
``` antiarrhythmics: Class III (Sotalol) Class IA (Quinidine) ```
303
Drug rxn: agranulocytosis
``` Clozapine Carbamazepine Colchicine Propylthiouracil Methimazole Dapsone ```
304
Drug rxn: aplastic anemia
``` Chloramphenicol Benzene NSAIDs Propylthiouracil Methimazole ```
305
Drug rxn: Direct Coombs-positive hemolytic anemia
Methyldopa | Penicillin
306
Drug rxn: gray baby syndrome
Chloramphenicol
307
Drug rxn: hemolysis in G6PD-deficient patients (6)
``` Isoniazid (INH) Sulfonamides Primaquine Aspirin Ibuprofen Nitrofurantoin ```
308
Drug rxn: megaloblastic anemia
Phenytoin Methotrexate Sulfa drugs
309
Drug rxn: thrombotic complications
OCPs (estrogens)
310
Drug rxn: cough
ACE inhibitors Use ARBs - no cough
311
Drug rxn: pulmonary fibrosis
Bleomycin Amiodarone Busulfan
312
Drug rxn: acute cholestatic hepatitis, jaundice
Erythromycin
313
Drug rxn: focal to massive hepatic necrosis
Halothane Amanita phalloides (death cap mushroom) Valproic acid Acetaminophen
314
Drug rxn: hepatitis
INH
315
Drug rxn: pseudomembranous colitis
Clindamycin | Ampicillin
316
Drug rxn: adrenocortical insufficiency
Glucocorticoid withdrawal (HPA suppression)
317
Drug rxn: gynecomastia
``` Spironolactone Digitalis Ciimetidine chronic Alcohol use estrogens Ketoconazole ```
318
Drug rxn: hot flashes (2)
Tamoxifen | Clomiphene
319
Drug rxn: hyperglycemia (5)
``` Niacin Protease inhibitors HCTZ Corticosteroids Tacrolimus (immunosupressant for transplants; eczema-atopic dermatitis) ```
320
Drug rxn: hypothyroidism (3)
Lithium Amiodarone Sulfonamides
321
Drug rxn: fat redistribution (2)
Glucocorticoids | Protease inhibitors
322
Drug rxn: gingival hyperplasia (2)
Phenytoin | Verapamil
323
Drug rxn: gout (4)
Furosemide Thiazides Niacin Cyclosporine (immunosuppressant)
324
Drug rxn: myopathies
``` Fibrates Niacin Colchicine Hydroxychloroquine Interferon-alpha Penicillamine Statins Glucocorticoids ```
325
Drug rxn: osteoporosis
Corticosteroids | Heparin
326
Drug rxn: photosensitivity
Sulfonamides Amiodarone Tetracycline
327
Drug rxn: rash (Stevens-Johnson syndrome)
``` Penicillin Ethosuximide Carbamazepine Sulfa drugs Lamotrigine Allopurinol Phenytoin Phenobarbital ```
328
Drug rxn: SLE-like syndrome
Hydralazine Procainamide Phenytoin INH SLE-like syndrome: Joint pain & muscle pain Inflammation of heart & lungs (pericarditis & pleuritis) Anti-histone antibodies
329
Drug rxn: teeth (kids)
Tetracyclines
330
Drug rxn: tendonitis, tendon rupture, cartilage damage
Fluoroquinolones
331
Drug rxn: diabetes insipidus
Lithium | Demeclocycline
332
Drug rxn: Fanconi's syndrome
Expired tetracycline Fanconi's syndrome: glucose, aa, uric acid, phosphate, bicarbonate passed in urine (instead of being reabsorbed)
333
Drug rxn: hemorrhagic cystitis
Cyclophosphamide Ifosfamide - treats testicular cancer Prevent by administering w/ mesna
334
Drug rxn: interstitial nephritis
Methicillin NSAIDs Furosemide
335
Drug rxn: SIADH
Carbamazepine | Cyclophosphamide
336
Drug rxn: Cinchonism
Quinidine | Quinine
337
Drug rxn: Parkinson-like syndrome
Antipsychotics Reserpine Metoclopramide
338
Drug rxn: Seizures
``` Isoniazid Bupropion Imipenem/cilistatin Tramadol Enflurane Metoclopramide ```
339
Drug rxn: Tardive dyskinesia
Antipsychotics
340
Drug rxn: antimuscarinic
Atropine TCAs H1 blockers neuroleptics
341
Drug rxn: disulfiram-like reaction
Metronidazole certain Cephalosporins Procarbazine 1st gen sulfonylureas
342
Drug rxn: nephrotoxicity/ototoxicity
Aminoglycosides Vancomycin Loop diuretics Cisplatin

STEP1 - TLe (8 decks)

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