Pharmacology Flashcards
1
Q
Captopril class
A
ACE inhibitor
2
Q
Verapamil class
A
Ca channel blocker
3
Q
Brimonidine (Alphagan)
A
Alpha 2 agonist
4
Q
Bethanechol (Urecholine)
A
Direct acting cholinergic agonist
5
Q
Methylphenidate (Ritalin)
A
Stimulant used in ADHD
Same function as amphetamine
6
Q
Betaxolol (Betoptic)
A
Beta-1 Blocker
1 blocker; tx glaucoma in asthmatics; Tx: HTN and angina
7
Q
When are beta blockers used?
A
Acute MI, CHF, HTN, arrhythmia, angina
8
Q
Cocaine
A
Inhibits DA and NE re-uptake into terminals has amphetamine-like effect but shorter acting and more intense
Severe HTN and stroke, tachycardia
Used for nasal surgery to decrease blood flow
9
Q
Succinylcholine (Anectine)
A
Depolarizing NMJ Blocker
initial stimulation and contraction→blockade; rapid procedures;
Phase I –prolonged depolarization, NO Reversal w/ AchE inh., makes it worse;
Phase II:AchE inh works;
SE: hypercalcemia, hyperkalemia-K+release(cardiac arrest – in burn/trauma pts), muscle pain
10
Q
Amlodipine class
A
Ca channel blocker
11
Q
Phenylephrine (Neo-Synephrine: Sudafed PE)
A
Alpha agonist
α1 selective agonist; use in hypotensive emergency; produces mydriasis, nasal decongestant(rebound), contracts prostate and GU spinchters
12
Q
Contraindications for beta blockers
A
Sinus bradycardia, heart block greater than first degree, sick sinus syndrome, cardiogenic shock, decompensated heart failure, asthma, COPD
13
Q
Tropicamide (Mydriacil)
A
Cholinergic (muscarinic) Antagonist
short-acting mydriasis and cycloplegia for eye examinations
14
Q
Nifedipine class
A
Ca channel blocker
15
Q
Cisatracurium (Nimbex)
A
Non-Depolarizing NMJ Blocker
Use: surgery- paralysis, mechanical ventilation, selective for motor nicotinic receptors, Reverse with neostigmine or edrophonium
Most commonly used (least toxic)
16
Q
Clonidine
A
Centrally acting alpha-2 agonist reduces sympathetic outflow and causes vasodilation and decreased CO for lower BP
selective α2 agonist; transdermal patch; tx for HTN, safe in renal disease; reduces craving in addicts, ↓ hot flashes
17
Q
Altracurium (Tracium)
A
Non-Depolarizing NMJ Blocker
18
Q
Nicotine
A
Direct acting cholinergic agonist
Selective for Nicotinic receptors;NMJ intial stim paralysis; Tx Atropine
19
Q
Prazosin (Minipress)
A
Alpha-1 selective blocker
selective for α1; lack of α2 block reduces likelihood of reflex tachycardia;
Tx: BPH and HTN Tox: 1st dose orthostatic hypotension; CI: w/ Viagra
20
Q
Terbutaline (Brethine)
A
Beta 2 agonist
Selective ß2 agonist; reduce premature uterine contractions
21
Q
Echothiophate
A
Cholinesterase Inhibitors
instill directly into eye; tx glaucoma in emergency; long action
22
Q
Tyramine
A
Indirectly increases release of catecholamines from nerve terminals
Replaces NE in vesicles with octopamine
Normally hydrolyzed by MOA in the gut and therefore inactive when given orally
Normal component of many foods
23
Q
Dobutamine (Dobutrex)
A
Beta 1 agonist
selective ß1 agonist, inotropic and chronotropic; cardiac stress test, heart failure, increase renin release
24
Q
Norepinephrine (Levophed)
A
Catecholamine
stimulate α=ß1»ß2; severe vasoconstriction at infusion site→ necrosis, tx: hypotension; effects ↑systolic, ↑diastolic ↑ MAP, no change in PP reflex ↓HR (ganglion blockers stop reflex bradycardia)
↓ = depression; pain regulation
25
Organophosphate pesticides
Cholinesterase Inhibitors
26
Metoprolol (Lopressor)
Beta-1 Blocker
1 blocker; inc. life post-MI; decrease renin; better exercise tolerance and in diabetics; risky in asthma(Use Ca++ channel blkrs in asthmatics)
27
Aliskiren class
Renin inhibitor
28
Carbachol (Isopto Carbachol)
Direct acting cholinergic agonist
| Glaucoma, pupillary contraction, relieves intraocular pressure
29
Phenoxybenzamine (Dibenzyline)
Alpha receptor blocker
Irreversible non-competitive antagonist at α1 and α2 ;tx: pheochromocytoma use pre surgery cuz catecholamines cant overcome noncompetitive inhibitor; SE: hypotension and tachycardia
30
Phentolamine (Regitine)
Alpha receptor blocker
Reversible competitive antagonist at α1 and α2; tx pt on MAO-I who ingest tyramine (HTN crisis); SE: release of Histmaine from Mast cells = gastric acid secretion PUD
31
Acebutolol (sectral)
Beta Blocker with intrinsic sympathetic activity
| selective ß1 antagonist w/ ISA; risk of bradycardia decreased
32
Glycopyrrolate (Rubinul)
Cholinergic (muscarinic) Antagonist
used in surgery to ↓ vagal response as well as decrease respiratory and other secretions;
Also decreases gastric acid secretion to treat PUD
Decrease side effects in tx of MG with Neostigmine and anytime Neostigmine is used after surgery
33
Albuterol (Ventolin)
Beta 2 agonist
| selective ß2 agonist; tx asthma, relax skeletal mm BV, promote K uptake
34
Losartan class
ARB
35
What category of drugs are the -prils? Example: Captopril
ACE inhibitors
Common side effect of ACEI's is coughing from decreased bradykinin breakdown
First line treatments for HTN in DM, Renal Disease, LVH
CI in pregnancy, causes acute renal failure in patients with renal artery stenosis, causes hyperkalemia
36
Enalapril
ACE inhibitor
Common side effect of ACEI's is coughing
First line treatments for HTN in DM, Renal Disease, LVH, congestive heart failure
CI in pregnancy, causes acute renal failure in patients with renal artery stenosis, causes hyperkalemia
37
Apraclonidine (Iopidine)
Alpha 2 agonist
| Selective α2 agonist used in eye to tx intraocular pressure by ↓ fluid
38
Donepezil (Aricept)
Cholinesterase Inhibitors
| Alzheimer’s disease; similar drug is Tacrine(severely hepatotoxic)
39
Adverse effects of beta blockers
Bradycardia, dizziness, HA, fatigue, hypotension, fainting, sexual dysfunction, bronchospasm
40
Chlorthalidone
Thiazide diuretic
| Prevents Na reabsoprtion in early distal tubule
41
Rocuronium (Zemuron)
Non-Depolarizing NMJ Blocker
42
Pindolol (Visken)
Beta Blocker with intrinsic sympathetic activity
| nonselective β blocker with some ISA; Tx: HTN and angina
43
Varenicline (Chantix)
Direct acting cholinergic agonist
| Partial agonist at Nicotinic Receptors(in the brain) N/V, Constipation, Vivid nightmares, psychosis
44
Amphetamine
Indirect acting sympathomimetic
Displaces NE and DA from vesicles increasing their release
CNS stimulant
Strong external urinary sphincter contractor
Releases stored catecholamines, blocks reuptake, CNS stimulant; tachycardia, HTN, psychosis ; uses : narcolepsy, obesity, ADD
45
Side effects of Clonidine
Centrally acting alpha-2 agonist
Hypotension, dry mouth, somnolence, fatigue, constipation, dizziness
Rebound HTN possible when discontinue use
46
Candesartan class
ARB
47
Pilocarpine (Isopto Carpine; Pilocar)
Direct acting cholinergic agonist
tx glaucoma; Contracts ciliary muscle of eye (open angle), pupillary sphincter (narrow angle); sweat and salivate excessively; SE; blurred vision
48
Carvedilol (Coreg)
Combined alpha and beta blocker
| ß-blocker and α1 blocker; decreases free radicals; tx HTN/CHF, post-MI
49
Oxybutynin (Ditropan)
Cholinergic (muscarinic) Antagonist
| prevent bladder spasm after prostate surgery
50
Diltiazem class
Ca channel blocker
51
What are the first line drugs used for depression?
SSRI's are the first-line drugs especially for those with suicidal ideation
Examples: fluoxetine, paroxetine, citalopram, sertraline
52
Oxymetazoline (Afrin)
Alpha agonist
53
Neostigmine (Prostigmin)
Cholinesterase Inhibitors
| Not X BBB; tx myasthenia gravis, post op and neurogenic ileus, reverse NMJ block
54
Tolterodine (Detrol)
Cholinergic (muscarinic) Antagonist
| Selective M3 – tx overactive bladder
55
Propranolol (Inderol)
Beta-receptor blocker
non-selective competitive antagonist; tx, HTN, post-MI, angina, arrhythmias, CHF, hyperthyroidism, stage-fright; DO NOT discontinue abruptly(up-reg of receptors)
56
Ipratropium (Atrovent)
Cholinergic (muscarinic) Antagonist
| inhalation for tx COPD and Asthma(blks Vaso-C)
57
Scopolamine
Cholinergic (muscarinic) Antagonist
| patch tx motion sickness; Penetrates CNS; SE:sedation/amensia
58
Nebivolol (Bystolic)
Beta-1 Blocker
| Most selective 1 blocker; Vaso-D due NO from endothelium; reduces cholesterol, TG’s and blood glucose
59
Physostigmine (Eserine)
Cholinesterase Inhibitors
instill directly into eye, crosses BBB; tx glaucoma, atropine poisoning
"phyxes" atropine overdose
60
Cevimeline (Evoxac)
Direct acting cholinergic agonist
| Selective for M3 receptors – salivation Not sweating
61
Acetylcholine (Miochol)
Direct acting cholinergic agonist
M and N receptors
No clinical use
acts on M and N receptors; memory, cognition, attention; Ach neurons degenerate in Alzheimer’s(nucleus basalis & hippocampus); balances DA
62
Esmolol (Brevibloc)
Beta-1 Blocker
| 1 blocker very short duration of action; give IV; tx if unsure pt can handle beta blockers
63
Tetrahydrazoline (Visine)
Alpha agonist
64
Salmeterol (Serevent)
Beta 2 agonist
| selective ß2 agonist; tx asthma, relax skeletal mm BV, promote K uptake
65
What category of drugs are the -sartans? Example: Losartan
ARB's
Angiotensin Receptor Blockers
More specific than ACEI's with similar side effects except for cough and angioedema
66
Dicyclomine (Bentyl)
Cholinergic (muscarinic) Antagonist
67
Atropine
Cholinergic (muscarinic) Antagonist
early MI to decrease bradycardia or AV block, cholinesterase inhibitor posining; SE: ↑pupil dilation, cycloplegia ↓airway secretion ↓gastric acid secretion ↓GI motility ↓urgency in cystitis ↑body temp (due to ↓sweating) Other SE(dose-dependent): dry mouth/skin ↑HR blurred vision/palpitations GI effects Delerium, Think “Hot as a hare, dry as a bone, red as a beet, mad as a hatter”
68
Nicardipine class
Ca channel blocker
69
Isoproterenol (Isuprel)
Catecholamine
ß1 and ß2 agonist; emergency tx of cardiac arrest (AV block) effects: no change/slight decrease in systolic, ↓diastolic, ↓MAP, reflex ↑HR
70
Epinephrine (Adrenaline)
Catecholamine
low dose selective for ß1 (looks like isoproterenol), high dose all adrenergic receptors; tx anaphylactic shock, cardiac arrest & complete heart blk, glaucoma; ß2 – cause Broncho-D
effects: ↑Systolic, ↓Diastolic, no change in MAP, ↑ Pulse Pressure, reflex ↑HR (due to ↓ diastolic) CI: in pts on β-Blkrs
71
Clonidine (Catapres)
Alpha 2 agonist
72
Mecamylamine (Inversine)
Ganglion Blocker
Rarely used
nicotinic agonist effects like blocking both sympathetic and parasympathetic input; prevents vagal reflex responses to changes in blood pressure, i.e. prevents reflex bradycardia caused by NE;
SE: cycloplegia, mydriasis, blurred vision, orthostatic hypotension, tachycardia, urinary retention, sexual dysfunction
73
Edrophonium (Tensilon)
Cholinesterase Inhibitors
binds reversibly; IV; Dx of myasthenia gravis; drug titration – strength increases to a point, then decreases; short action
74
Bethanechol
Cholinergic Agonist
| Selective muscarinic receptors, stimulate peristalsis and urination, for post operative and neurogenic ileus
75
d-Tubocurarine
Non-Depolarizing NMJ Blocker
Use: surgery- paralysis, mechanical ventilation, selective for motor nicotinic receptors, Reverse with neostigmine or edrophonium
histamine release leads to hypotension + Bronchospasm
76
Tamsulosin (Flomax)
Alpha-1 selective blocker
| selective for α1A; tx BPH w/ little effect on BP; SE:↓ejaculation
77
Sotalol (Betapace)
Beta-receptor blocker
78
Ephedrine
Alpha, Beta agonist and increases NE release
Similar effects to epinephrine but not as pronounced
Releases stored catecholamines, has direct action; uses: nasal decongestant, urinary incontinence, hypotension
79
Solifenacin (Vesicare)
Cholinergic (muscarinic) Antagonist
| Selective M3 – tx overactive bladder
80
Hexamethonium
Ganglion Blocker
Rarely used
nicotinic agonist effects like blocking both sympathetic and parasympathetic input; prevents vagal reflex responses to changes in blood pressure, i.e. prevents reflex bradycardia caused by NE;
SE: cycloplegia, mydriasis, blurred vision, orthostatic hypotension, tachycardia, urinary retention, sexual dysfunction
81
Reserpine
Causes depletion of NE, DA, 5-HT
| No longer used
82
Pancuronium
Non-Depolarizing NMJ Blocker
Use: surgery- paralysis, mechanical ventilation, selective for motor nicotinic receptors, Reverse with neostigmine or edrophonium
vagal blockade and tachycardia
83
Methacholine
Cholinergic agonist
| Dx of Asthma – stims M recetors in airway when inhaled
84
Pyridostigmine
Cholinesterase Inhibitor
| Myasthenia gravis, long acting, does not penetrate CNS
85
Pralidoxime (2 PAM)
early tx organophosphate poisoning; CI: Carbamates(don’t age)
86
What are the SSx of organophosphate poisoning and how is it treated?
DUMBBELSS
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardis, Excitation of skeletal muscles and CNS, Lacrimation, Sweating, Salivation
Tx: atropine + pralidoxime (2-PAM) before the aging process
87
Methscopolamine
Cholinergic Antagonist
| Peptic Ulcer Treatment
88
Dyphenoxylate-atropine (Lomotil)
Cholinergic Antagonist
| Combo of opoid and atropine to treat Diarrhea
89
Benztropine
Cholinergic Antagonist
| decrease extrapyramidal symptoms of antipsychotics; Parkinson’s
90
Vecuronium
Non-Depolarizing Neuromuscular Blockers
Use: surgery- paralysis, mechanical ventilation, selective for motor nicotinic receptors, Reverse with neostigmine or edrophonium
liver metab; duration 20-40mins
91
Rocuronium
Non-Depolarizing Neuromuscular Blockers
Use: surgery- paralysis, mechanical ventilation, selective for motor nicotinic receptors, Reverse with neostigmine or edrophonium
intubation (rapid onset)
92
Dopamine
Catecholamine
low dose activate D1, high dose ß1 on heart; tx cardiac shock w/o VasoC
addiction, emotions, movement; Nigro-striatal DA neuron degeneration in Parkinson’s; excess = psychosis, schizophrenia
93
Alpha-methyldopa
Selective α2 agonist; Same as clonidine but safe in pregos
94
Ritrodine
Selective ß2 agonist; reduce premature uterine contractions
95
How do beta 2 receptors influence aqueous humor production?
Beta-2 receptors increase production of aqueous humor leading to increased IOP
96
Fendolapam
Selective D1 agonist; dilation of vascular beds
| Tx severe HTN rapidly
97
What drug causes orange colored urine and what is it used to treat?
Rifampin
| TB
98
What are the 4 first-line drugs for TB?
Isoniazid, Rifampin, Ethambutol, Pyrazinamide
99
Isoniazid
Treatment for TB, inhibits P450, can cause Vit B6 deficiency, hepatitis, peripheral neuropathy
100
Rifampin
Treatment for TB, orange colored urine, inhibits DNA dependent RNA polymerase, induces P450, hepatotoxic
101
Ethambutol
Treatment for TB, causes color blindness and decreased visual acuity
102
Pyrazinamide
Treatment for TB, causes non-gouty arthralgia
103
Common P450 inducers
```
Rifampin
Phenobarbitol
Carbamazepine
Phenytoin
St. John's wart
Corticosteroids
Efavirenz
Pioglitazone
```
104
Common P450 inhibitors
```
Isoniazid
Cimetidine
Azole antifungals
Erythromycin
Grapefruit juice
SSRI's
```
105
What are common toxicities from aminoglycosides like Streptomycin?
Ototoxicity
| Nephrotoxicity
106
Terazosin, Doxazosin
Alpha receptor blocker
selective for α1; lack of α2 block reduces likelihood of reflex tachycardia; Tx: BPH and HTN Tox: 1st dose orthostatic hypotension; CI: w/ Viagra
107
Yohimbine
α2 selective antagonist; increases NE release; acts opposite Clonidine
108
Mirtazapine
α2 selective antagonist; use: depression w/ insomnia; SE: sedation, inc. serum cholesterol, inc. appetite
109
Timolol
Beta Blocker
| non-selective competitive antagonist; tx glaucoma(↓ aqueous humor production; CI: asthmatics
110
Labetalol
Beta Blocker
| blocks ß1 ß2 and α1; IV tx hypertensive emergency; SE: liver injury
111
Guanethidine
Replaces NE in vesicles decreasing its release
| Used for HTN
112
Reserpine
```
Antipsychotic, anti HTN
Inhibits VMAT
Decreases catecholamines
Increases cholinergic effects in body–ANS, GI, BV, smooth muscle
Not used much
```
113
Metyrosine
blocks tyrosine hydroxylase, ↓synthesis of catecholamines; pre-surgical tx of pheochromocytoma
114
Serotonin
decrease=depression, anxiety; excess = sleep; raphe nuc to limbic
115
GABA
major inhibitory in CNS, interneurons; ↑=anxiety relief; ↓ = seizures (↑NMDA activity)
GABAA - ↑Cl conductance (Barbs, Benzos, EtOH)
GABAB - ↑K, ↓Ca conductance (Baclofen)
116
Glutamate
major excitatory in CNS; inotropic, metabotropic; etoh blocks @ NMDA; NMDA receptor(glycine must bind) – learning, memory, long
term potentiation; ↑Glutamate = seizures
117
Glycine
inhibitory; brain stem & spinal cord interneurons; blocked by strychnine
118
Neuropeptides
endogenous opiates; endorphins, enkephalin, substance P
119
Cannabinoids
THC; memory, cognition, pain
120
What causes Parkinson's?
Nigrostriatal dopaminergic neurons - SN to caudate/putamen (part of striatum); degeneration → ↓DA (& relative ↑Ach activity) → Parkinson’s
121
DA metabolism
tyrosine → l-dopa (dopa decarboxylase) → dopamine (MAO-B & COMT) → HVA; DA doesn’t cross BBB, l-dopa does cross BBB
122
L-Dopa (Levodopa)
Parkinson's drug
symptomatic relief only; greatly metabolized in GI and periphery →nausea and vomiting, vasodialte(↑ DA receptor axn)
DA doesn’t cross BBB, l-dopa does cross BBB
123
Carbidopa/Levodopa
Parkinson's Drugs
carbidopa: inh dopa decarboxylase; carbidopa does not cross BBB; ↑ l-dopa entry into brain→↓ dose required; ↓peripheral effects; ↓effectiveness w/ time (3-4 years) due to continued loss of DA neurons;
SE: nausea, postural hypotension, psychosis***(tx w/ clozapine, aripiprazole), insomnia, dyskinesia; Rapid withdrawal = NMS; Intraxn: MAOI’s → hypertensive crisis; CI: psychosis, malignant melanoma
124
Selegiline
Parkinson's Drug
inh MAO-B dopamine availability; ↓ROS, may slow disease progression; used w/ l-dopa/carbidopa; insomnia; CI: w/ meperidine
125
Bromocriptine
Parkinson's Drug
| direct DA receptor agonist→ effectiveness does not ↓ with time; SE: erythromelalgia – red, tender, swollen feet
126
Pramipexole, Ropinirole
Parkinson's Drugs
| DA receptor agonist; well tolerated, initial tx; ↓ restless legs SE: sudden sleep
127
Amantadine
Parkinson's Drug
| antiviral; may ↑ DA release; SE: psychosis, seizures, spotting of skin; reddish blue spots on body
128
Benztropine
Parkinson's Drug
| anti-muscarinic; restores DA-Ach balance; ↓ tremor, ↓ rigidity; little effect on bradykinesia
129
Tolcapone
Parkinson's Drug
| COMT Inhibitors – prevent L-dopa degradation, dopamine available; Not as good as Selegiline. SE: liver disease
130
What NT changes occur in Alzheimer's?
Confusion, memory loss, personality changes → anxiety, difficulty recognizing family/friends → loss of speech, appetite, bladder control
Degeneration of cholinergic neurons – nuc basalis of Meynert to cerebral cortex & hippocampus; ↓Ach levels; eventual ↓ in NE & 5HT
131
Memantine
Alzheimer drug
NMDA antagonist – prevents glutamate neurotoxicity→ may slow disease progression; SE: dizziness, confusion, hallucinations, mostly urinary
132
Donepezil, Tacrine, Rivastigmine, Galantamine
```
Alzheimer drugs
cross BBB (diff. from, eg, neostigmine), Inhibit AChE in the brain; GI SEs, nausea, dizziness(Tacrine Liver probs)
```
133
Barbiturate characteristics
Bind GABAA, enhance axn independent of GABA(prolongs opening of Cl- channel); hypnosis; Low safety margin; life threatening withdrawal; schedule II of III; synergy w/ EtOH; Cyp450 inducer
SE: CNS depression, mood distortion, ↓respiratory drive, ↓BP, ↓REM sleep; CI: porphyria
Tx of OD: diuresis/alkalinization of urine, don’t give stimulant; SUPRA-additive w/ other CNS depressants
134
Phenobarbital
Barbiturate
| Long acting, anticonvulsant
135
Phenobarbital
Barbiturate
136
Thiopental
Barbiturate
| Ultra short acting, anesthesia induction
137
Secobarbitol
Barbiturate
138
Benzodiazapines cahracteristics
Bind GABAA complex, enhance axn only when GABA is present → ceiling effect, relatively safe; liver met (no Cyp); synergy w/ EtOH;
Eff: anti-anxiety, sedation, muscle relax(diazepam), anticonvulsant, NO CNS Depression(Barbits)
SE: dizziness, drowsiness, sedation, memory loss; esp. in elderly
Tolerance: when used chronically, discontinuation → insomnia, anxiety, seizures
CI: pregnancy, children, sleep apnea, not great in elderly
Tx: anxiety except OCD(w/SSRIs), PTSD(anti-D), agoraphobia(w/SSRIs), children(anti-D)
139
Diazepam (Valium)
Benzodiazepine
| long T1/2; tx: status epilepticus, alcohol/barbs withdrawal, muscle spasm/relaxant
140
Chlordiazepoxide
Benzodiazepine
| long T1/2; tx: alcohol/barbs withdrawal(tapered)
141
Lorazepam
Benzodiazepine
| int T1/2(
142
Clonazepam
Benzodiazepine
| Tx Absence seizures
143
Flurazepam
Benzodiazepine
| Long T1/2 = 74hrs; hypnotic; SE “hang over”
144
Alprazolam
Benzodiazepine
| short T1/2; anxiety + depression
145
Midazolam (Versed)
Benzodiazepine
| very short T1/2; anterograde amnesia in surgery, IV
146
Temazepam, Triazolam
Benzodiazepine
| Short acting hypnotic (rebound insomnia)
147
Oxazepam
Benzodiazepine
| Short acting
148
Flumazenil
Benzo antagonist, IV only, reverse effects of above and below; may cause seizures w/ chronic Benzo/Barbs/TCAs
149
When are Benzos not used and what is used instead?
OCD (SSRI)
Panic (SSRI)
PTSD (antidepressant)
Anxiety in kids (antidepressant)
150
Zolpidem, Zaleplon
Bind to BZ1 subtype of GABA, causes sleep, rapid short action
SE: “blackouts,” amnesia, rebound insomnia, sleep driving, eating,
151
Eszopiclone
Similar to Zolpidem(longer), activates all BZ receptors
| Anti-anxiety and sedative
152
Ramelteon
Sedative
| Melatonin receptor agonist, no dependence or rebound
153
Buspirone
5HT1A partial agonist; tx: anxiety w/out causing sedation; 2 weeks for effect; very low addiction potential no GABA effect; little to no sedation; no interaction w/ EtOH, benzos; Intraxn: ↑BP with MAOI’s
154
Ethanol
GABAA is down-regulated & NMDA is up regulated with chronic use; causes sedation but decrease quality of sleep; Zero Order – 10g metabolized/hr(means a 12oz beer takes one hour to metabolize); Vaso- D hypothermia, ↓ADH effect diuretic
155
Disulfiram
Inh aldehyde dehydrogenase
156
Naltrexone
Treatment for alcohol
| Blks reward pathway(β-endorphins are blkd from working on opioid receptors)
157
Acamprosate
Alcohol treatment
| Analogue of GABA; restores normal balance of GABA and glutamate
158
General MOA of CNS stimulants
↑DA (& NE) levels
Effects – Low dose: ↑BP, ↑alertness, ↓appetite, euphoria
Med dose: tremor, restlessness, ↑respiration
High dose: behavioral repetition, psychosis Physical dependence, abuse potential
159
Methylphenidate (ritalin, Concerta)
CNS Stimulant
| tx: ADHD, narcolepsy, obesity
160
Amphetamine (Adderall)
CNS Stimulant
| tx: ADHD, narcolepsy, obesity; causes NE release
161
Atomoxetine (Strattera)
CNS Stimulant
| SNRI, (-)NE reuptake; tx: ADHD ; no abuse potential
162
Caffeine
CNS Stimulant
blocks adenosine receptors, (-)PDE→ ↑cAMP; Eff: ↑alertness, ↑ gastric acid, diuresis vaso-C cerebral BV’s→ headache relief; High dose: tachy,
hypertension, insomnia
163
Cocaine as CNS stimulant
CNS stimulant
| inhibits NE re-uptake
164
Baclofen
Centrally acting muscle relaxant
Agonist at GABAB (inh Ca++ channels presynaptically and opens K+ postsynaptically hyperpolarizes and inh NT release; Can also inh substance P(relieving pain)
165
Diazepam
Centrally acting muscle relaxant
| Acts on GABAA in the spinal cord to decrease spasticity
166
Cyclobenzaprine (Flexeril)
Centrally acting muscle relaxants
| Tx acute muscle spasm
167
Carisoprodol
Centrally acting muscle relaxants
| Central sedative
168
Tizanidine
Centrally acting muscle relaxants
| Agonist at α2 presynaptically reducing spasm
169
Dantrolene
Centrally acting muscle relaxants
| Interferes w/ Ca++ release from SR; Tx malignant Hyperthermia
170
Botulinum Toxin
Centrally acting muscle relaxants
171
Physical dependance
abnormal behavior and physical symptoms occur with withdrawal(not indicate addiction)
172
Psychological dependance
Dysphoria and intense craving following withdrawal.(drive to avoid discomfort)
173
Cocaine as drug of abuse
inhibits DA and NE re-uptake; Local anesthetic, vaso-c, energy, euphoria, all sympathomimetic sxs; Paranoid Psychosis; Major Cardiac probs;
Taken IV/smoke(fast), nasal(long high), chewing (slight high); cocaine bugs, Slow recovery(1-2yrs); Intense psych dependence;
rapidBP↑=cerebral hemorrhage
174
Methamphetamine as drug of abuse
Release NE and DA, euphoria, energy, decreased appetite, increased BP, Cardiac toxic, high abuse, psychosis with weight loss, slow recovery, death by seizures, organ damage, stroke, heart attack, Meth bugs, toxic with ETOH
175
Nicotine as drug of abuse
Most addictive, increase 5HT and DA release, increase memory, learning, alertness; very reinforcing, inc BP and HR, mild stimulant
176
Alcohol as drug of abuse
withdrawal worst, CNS depressant
| Tx: naltrexone + Prozac
177
Benzos and Barbiturates as drugs of abuse
Combined with other drugs but rarely abused; CNS depressant, flunitrazepam-Rape
178
Opioids as drugs of abuse
Inc DA, euphoria, reduced anxiety, sedative, tolerance, abuse seen in health professionals, facilitate reward pathway
179
Marijuana (THC)
Least addictive of drugs of abuse
| mild euphoria, slows time, psych dependence, impairs short term memory, MEDS-anti-emetic, increase appetite, analgesia
180
LSD drug of abuse
Euphoria, visual hallucinations, bind 5HT2, bad trips/flashbacks, "shrooms"
181
Mescaline as drug of abuse
Similar to LSD but less potent
182
MDMA (Ecstasy)
Inc 5HT release, inc HR and BP, hyperthermia and dehydration, memory problems
183
Phencyclidine (PCP, angel dust)
NMDA receptor antagonist, analgesia (Ketamine is derivative), aggressive
184
Ketamine
NMDA receptor antagonist; "date rape", sense of floating
| Dissociative analgesia
185
TCA's
Inh reuptake of 5HT & NE; also block M, α, and H receptors
SE: sedation (H block), memory loss (Ach block), analgesia (↑NE), cardiotoxicity (Torsades), ↓seizure threshold convulsions, coma, α1 block – postural hypotension, reflex tachy, dry mouth; weight gain?, SIADH, sexual dysfunction, suicidal tendencies Drug Intraxn: MAOI’s → serotonin syndrome – hyperpyrexia, seizures, coma; wait 2-3 weeks after MAOI; SSRI’s - ↑TCA levels, toxicity; Amphetamine – hypertension; Cocaine – arrhythmias
Tx: depression, panic attacks, chronic pain, fibromyalgia, neuropathic pain(most common use), enuresis
186
Amitriptyline, Imipramine
TCA Antidepressant
| tertiary amine; more sedating; → active metabolite (Imipramine – tx enuresis)
187
Nortriptyline, Desipramine
TCA Antidepressant
| secondary amine; less sedating; active form, less anti-ACh effects that tertiary
188
MAOI's
Antidepressant
MAO-A breaks down 5HT and NE and tyramine
MAO-B breaks down DA
Tx: depression
SE: Hypertensive crisis with tyramine ingestion(in foods), also block α and m(same side effects as above)
189
Phenelzine (Nardil)
MAOI
| Antidepressant
190
Clomipranine
TCA used only for OCD, works like an SSRI
191
SSRI's
Inh 5HT reuptake; take 2-3 weeks for effect; mild SE’s
SE: GI upset, weight loss, CNS stimulation – anxiety, insomnia; sexual dysfunction, SIADH is possible, no ANS effects
Drug Intraxn: MAOI’s/St John’s Wart – serotonin syndrome; TCA’s - ↑TCA levels, toxicity; Opioids (w/ fluoxetine) - ↓ opioid effect
Tx: DOC depression, panic, OCD; agoraphobia, bulimia, alcoholism, kids
192
Fluoxetine (Prozac)
SSRI for depression
| very long T1/2, 5 weeks(and metabolite) to clear; inh Cyp2D6 (↓effect of codeine, hydrocodone, oxycodone), insomnia
193
Paroxetine (Paxil)
SSRI
| OCD, agoraphobia SE: sedation, inh cyp2D6; CI: Pregnant
194
Sertraline (Zoloft)
SSRI
| Safer than Fluoxetine w/ shorter duration of action
195
Citalopram (Celexa)
```
SSRI
faster onset (1-2 weeks)
```
196
Escitalopram (Lexapro)
SSRI
| Faster onset than citalopram
197
Venlafaxine (Effexor)
| Desvenlafaxine (Pritiq)
SNRI
| Inh 5HT & NE reuptake; tx: depression, more for chronic pain; more SE’s than SSRIs less than TCAs, ↑BP
198
Duloxetine (Cymbalta)
SNRI
| 5HT & NE reuptake, greater NE effect; tx: depression, neuropathic pain, hepatotoxic
199
Bupropion (Wellbutrin)
Antidepressant in other category
Inh Dopamine reuptake; tx: depression, ADHD, smoking cessation; less sexual dysfunction; can cause seizures, anxiety and insomnia at high doses, wt loss CI: pts w/ seizures or head trauma
200
Mirtazapine (Remeron)
Antidepressant in other category
blocks α2→↑5HT & NE but blocks 5HT2A, 3 receptors→ fewer SSRI SE’s (less sexual dysfunction); tx: depression w/ insomnia; SE: sedation, appetite, weight gain, dry mouth
201
Atomoxetine (Strattera)
Selective NE reuptake inh. Tx of ADHD
202
Trazodone (Desyrel)
partial agonist at 5HT1A & blocks 5HT2; tx: sleep aid, pain; SE: sedation, priapism
203
St. John's Wart
may block 5HT & NE reuptake; SE: metabolism of other drugs(anything w/ a small therapy range; careful), especially protease inhibitors
204
Schizophrenia
hallucinations, lack of affect, apathy, delusions;↑dopaminergic activity
205
Dopaminergic systems in brain
Nigrostriatal - SN to caudate/putamen (part of striatum); posture & movement; ↓ in activity → extrapyramidal symptoms (Parkinson’s)
Mesolimbic-Mesocortical – ventral tegmental area (midbrain) to limbic-nucleus accumbens (striatum)/frontal cortex; reward, emotions, cognition; ↑ activity → psychosis
Pituitary – Arcuate nuc (hypothalamus) to ant pituitary; inh prolactin secretion
D2 block for tx of “positive” symptoms - delusions
D4 & 5HT2A block for tx of “negative” symptoms – apathy
206
Typical antipsychotics
Most block D2, α, Muscarinic, and Histamine receptors
Effect: ↓ fear, ↓hallucinations, ↓anxiety, antiemetic
Extrapyramidal symptoms (EP’s) – akathisia, dystonia, tremor, tardive dyskinesia: tx by bringing dopamine and Ach activity into balance; so drugs with more anti-Ach have ↓EP symptoms
207
Tardive dyskinesia with antipsychotics
stereotypic oral facial movements probably due to dopamine receptor sensitation, after long term use
208
Common SE of antipsychotics
Other SE: Postural hypotension, dry mouth blurred vision, inhibition of ejaculation, sedation and weight gain(a lot), Neuroleptic syndrome(rare, tx: dantrolene), hyperprolactinemia, anti-m effects: dry mouth, constipation, hypotension, sedation
209
Thioridazine (Mellaril)
Phenothiazine antipsychotic blocks D2
| Low potency less EPS symptoms, retinal deposits
210
Fluphenazine (Prolixin)
Phenothiazine antipsychotic blocks D2
| High potency EPS symptoms
211
Trifluoperazine
Phenothiazine antipsychotic blocks D2
| High potency EPS symptoms
212
Chlorpromazine (Thorazine)
Phenothiazine antipsychotic blocks D2
| Low potency less EPS symptoms, corneal deposits, jaundice, tx N/V
213
Haloperidol (Haldol)
Conventional antipsychotic specific for D2
High potency causes worst EPS Sx of antipsychotics, no ACh effects, DOC – acute highly sedating
We can see here from the drug haloperidol that it is the block of the D2 receptors that are responsible for the EP symptoms.
Remember that you want to block the D2 receptors in the case of psychosis because too much DA will cause this problem. The goal of Tx is to bring the DA and ACh back into their proper ratios.
214
New generation/atypical antipsychotics
Block 5-HT2a, D4/D2, α, and H1 receptors
| Less EPS and anticholinergic effects, treat both positive and negative symptoms, all have wt gain (except aripiprazole)
215
Olanzapine (Zyprexa)
Atypical Antipsychotic
| Blks D4 Also used in OCD, anxiety, depression, Tourette’s SE: Weight gain, hyperglycemia(worst), Type II diabetes
216
Clozapine (Clozaril)
Atypical Antipsychotic
| Blks D4, no tardive or EPS, agranulocytosis
217
Quetiapine (Seroquel)
Atypical Antipsychotic
| No prolactin increase, SE: sedation, adjunct in depression tx
218
Risperidone (Risperdal)
Atypical Antipsychotic
| Lengthens QT interval (no use in elderly)
219
Ziprasidone (Geodon)
Atypical Antipsychotic
| Lengthens QT interval (no use in elderly)
220
Aripiprazole (Abilify)
Atypical Antipsychotic
blocks 5HT2A; partial agonist at D2 & 5HT1A; “dopamine stabilizer”; anti- anxiety, blk – and + Sxs;↓EP’s, ↓prolactin effects; SE: orthostatic hypotension, hyperglycemia, sedation, seizures, ↓esophageal motility
221
Lithium (Eskalith)
Mood stabilizer Tx for bipolar
kidney excretion, competes w/ Na for resorption; Thiazides, NSAID’s, & ↓Na→↑ [Li]; SE: nausea, headache, tremor, ↓thyroid function, edema, weight gain, diabetes insipidus (tx w/ amiloride); narrow therapeutic range; Toxicity: nausea, tremor, fasciculations →confusion, ataxia, seizures, arrhythmias, coma
222
```
Valproic acid (Depakene)
Divalproex (Depakote)
```
anticonvulsant and mood stabilizer; rapid onset blocks Na channels, increase GABA; monitor liver enzymes
223
Carbamazepine (Tegretol)
anticonvulsant and mood stabilizer, increase Na channel inactivation
224
Topiramate (Topamax)
anticonvulsant and mood stabilizer, blocks Na channels, increase GABA
225
Lamotrigine (Lamictal)
anticonvulsant and mood stabilizer, Block voltage gated Na channels
226
Gapapentin (Neurontin)
Mood stabilizer
| Tx pain; CI: pregnancy (not good for bipolar disorder)
227
Partial seizure
Partial: Simple – jerking, ~20 sec, preservation of consciousness
228
Complex seizure
impaired consciousness
229
Generalized seizure
Tonic-Clonic (Grand Mal) – loss of consciousness, muscle contractions
230
Absence (Petit Mal) seizure
staring, ~30 sec (low threshold Ca++ in Thalamus)
231
Possible cause of seizures and treatment strategy
Possible due to ↓GABA or ↑Glutamate (NMDA) activity – (tx: blk Na+ Channels and enhance GABA)
Most anticonvulsants are CI: pregnancy (most are teratogens)
232
Phenytoin (Dilantin)
Anticonvulsant
prolongs Na channel inactivation; Tx: partial & tonic-clonic seizures; Induces P450, ↑ [warfarin], ↑oral contraceptive metabolism, dose dependent elimination; SE: gingival hyperplasia, hirsutism, nystagmus, double vision
233
Carbamazepine (Tegretol)
Anticonvulsant
blocks Na channels; Tx: partial(DOC) & tonic-clonic seizures, trigeminal neuralgia, bipolar disorder; Drug intraxns, induces P450, SE: blood dyscrasias(anemia, agranulocytosis), GI upset;
234
Phenobarbitol (Luminal)
Anticonvulsant
| prolongs Cl- opening at GABA; Barbiturate; Tx: partial & tonic-clonic
235
Gapapentin (Neurontin)
Anticonvulsant
GABA analog but nebulous mech; Tx: adjunct for partial & tonic- clonic seizures, neuropathic pain, bipolar disorder; kidney excretion
236
Pregabalin (Lyrica)
tx: neuropathic pain, fibromyalgia
237
Topiramate (Topamax)
Anticonvulsant
| blocks Na, ↑GABA, ↓glutamate(less teratogenic)
238
Ethosuximab (Zarontin)
Anticonvulsant
| ↓Ca current in thalamus; Tx: absence seizures(DOC); SE: GI pain
239
Valproic Acid (Depakene)
Anticonvulsant
↓repetitive firing; Tx: absence + tonic-clonic(DOC), myoclonic, bipolar, migraine; SE: hepatotoxicity; Many drug intraxns
240
Clonazepam (Klonopin)
Benzo used for status epilepticus
241
Diazepam (Valium)
Benzo used for status epilepticus
242
Lorazepam (Ativan)
Benzo used for status epilepticus
243
Stevens-Johnson Syndrome and erythema multiform
Hypersensitivity autoimmune (immune complex) reaction; can happen w/ anticonvulsants; Epidermis separates from dermis; Tx: discontinue drug
Erythema multiforme, arthritis, nephritis, CNS abnormalities, myocarditis
DRUGS : Phenytoin, Carbamazepine, Oxcarbazapine, Phenobarbital, primordine, Lamtrigine, Tiagabine, Ethosuximide, Valproic Acid
244
Digitalis (foxglove, Digitalis purpurea, draft evaders, arrow poison)
Positive Inotropic agent
Inh Na/K-ATPase → ↑ IC Na (↓ IC K) → ↓ Ca expulsion so ↑ IC Ca → ↑ contractility, ↓ HR, ↑ CO & vaso-D in failing hearts only, ↓ AV conduction; Tx: CHF, A-fib, A-flutter
SE: GI upset → lower dose, cardiac (brady, AV block, bigeminy) → cease therapy; CNSToxicity: ↑ by Ca, ↓ by K; Tx toxicity w/ K or DigiBind for ODCI(relative): quinidine (↑ serum drug), K losing drugs, ß-blockers, cardioversion (except v-fib); T1/2= 40hrs(1wk until steady state)
245
Loop diuretics
Furosemide, torsemide, bumetanide, ethacrynic acid
| All sulfa drugs except for Ethacrynic acid which is most ototoxic
246
Acetazolamide (Diamox)
Carbonic Anhydrase inhibitor diuretic
| Oral tx for Acute Moutain sickness
247
Methazolamide (Neptazane)
Carbonic Anhydrase inhibitor diuretic
248
Brinzolamide (Azopt)
Carbonic Anhydrase inhibitor topical for glaucoma
249
Dorzolamide (Truspot)
Carbonic Anhydrase inhibitor topical for glaucoma
250
Thiazide + other diuretics
Indapamide, Metolazone, Hydrochlorothiazide
251
K-sparing diuretics
Inh Na/K exchange (collecting ducts) → ↑Na excretion, K sparing Hyper-K, acute renal failure Tx: CHF, combined with K losing drugs, cirrhosis
CI: Hyper-K
Triamterene, Amiloride (DOC for lithium induced DI), Spironolactone, Eplerenone
252
Aldosterone antagonists
Diuretics
inh. Aldosterone receptors in distal/collecting duct; Tx: edema assoc w/CHF, cirrhosis, nephrotic syndrome
- Spironolactone – ↑ survival in CHF, most effective in hyperaldosteronism; SE: gynecomastia
- Eplerenone – ↑ survival in CHF, ↓ endocrine SE’s, CYP3A4 met
253
B type natriuretic peptide
Nesiritide (Natrecor) – Tx: acute decompensated CHF; will ↓PCWP
254
Carbonic anhydrase inhibitor action for Diuresis
```
Inh CA (proximal tubule) → ↓ bicarb reabsorption, ↑ Na excretion due to lack of H+ in lumen ↑ K exc. in DCT and collecting duct. Tx: met alkalosis, acute mtn sickness, glaucoma, alkalinize urine CI: cirrhosis, sulfonamide hypersensitivity; Tox: renal sotnes, renal K+ wasting, hyperchloremic metabolic acidosis
Effective for only a few days
```
255
Loop diuretic MOA
| high Na+ excretion
Blk Na-K-2Cl cotransport (thick asc. loop)→ ↑Na, K, Mg, Ca, H+ excretion Reducing concentration gradient in the renal medulla imparing concentration and diluting capacity of kidney.
SE: OH DANG! – Ototoxicity, Hypokalemia, Dehydration, Allergy(sulfa), Nephritis(interstitial), Gout
Tx: CHF, pulm edema, acute renal failure, hyper-K, hyper-Ca, CI: avoid NSAIDs
256
Thiazide diuretics MOA
Inh Na/Cl reabsorption (distal diluting site) → ↑Na, K, Cl excretion; ↑Ca++ reabsorption; Tx: HTN, CHF, nephrolithiasis, Nephrogenic DI Tox: Hypo-K, met alkalosis, Ca sparing (↓ stones), hyperglycemia(may ↓ release of insulin- Type II DM), hyperlipidemia, hyperuricemia, liver metabolism, Sulfa allergy
257
Osmotic Diuretics
Increased osmotic activity, water retention (prox, loop, CD) (freely filterable agents)
Dehydration, hyper-Na
CI: severe CHF (early over-expansion of intravascular space)
Mannitol
258
Desmopressin
ADH agonist, strong V2 agonist, increases factor VIII and vWF
259
Vasopressin
ADH agonist
260
Demeclocycline
ADH antagonist, produces nephrogenic DI, SE: hyponatremia
261
Lithium and diuresis
ADH antagonist, produces nephrogenic DI, SE: hyponatremia
262
Conivaptan, Tolvaptan
V1 and V2 vasopression receptor antagonists; ↑urine output
263
Methyclothiazide (Enduron)
Thiazide diuretic
264
HMG-CoA reductase Inh “statins”
Lovastatin – blk rate limiting step in cholesterol synthesis; most effective in heterozygous familial hypercholesterolemia or combined hyperlipoproteinemia; CI: pregnancy
265
Pravastatin (Pravachol)
HMG-CoA reductase Inh
266
Simvastatin (Zocor)
HMG-CoA reductase Inh
267
Fluvastatin (Lescol)
HMG-CoA reductase Inh
268
Atorvastatin (Lipitor)
HMG-CoA reductase Inh
269
Rosuvastatin (Crestor)
HMG-CoA reductase Inh
270
Pitavastatin (Livalo)
HMG-CoA reductase Inh
271
Cholestyramine (Questran)
Bile acid binding resin; inh reabsorption of bile acids from the gut ↑LDL receptor expression in the liver; NOT effective in homozygous familial hyperlipidemia(no LDL receptors); SE: tastes horrible, GI-constipation and bloating, ↓ absorption of fat-soluble vitamins and Cholesterol gallstones; Impair absorption of digitalis, thiazides, tetracycline, thyroxine or ASA
Similar: Colestipol (Colestid), Colesevelam (WelChol)
272
Nicotinic Acid (Niacin)
Inh the secretion of VLDL from the liver, ↑HDL; Most effective in heterozygous familial hypercholesterolemia(combo wil bile-acid binding resins), also in familial combined hyperlipoproteinemia, familial dysbetalipoproteinemia, hypercholesterolemia
273
“Fibrates” -Gemfibrozil -Fenofibrate
Ligand for PPAR-α: Stimulate Lipoprotein lipase to increase hydrolysis of VLDL; SE: Myositis, hepatotoxicity, cholesterol gallstones
Effective in: familial dysbetalipoproteinemia and hyperTG NOT effective: primary chylomicronemia and familial hypercholesterolemia
274
Ezetimibe (Zetia)
Inh the absorption of dietary and biliary cholesterol from the intestine.
275
Orlistat (Xenical)
Wt loss; inh pancreatic lipase; SE: oily stool
276
Alirocumab, Evolocumab
Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors used for high cholesterol/lipid
277
What are the general treatment modalities for angina?
Nitrates/Nitrites for vasodilation
Ca channel blockers for vasodilation, decrease HR
Beta Blockers to reduce O2 demand on heart
Phosphodiesterase-5 inhibitors to vasodilate
278
Nitrates and Nitrites for angina
Nitrates and Nitrites – sublingual
Most effect on veins(↓preload) also redistributes coronary blood flow; nitrite ion →NO →↑cGMP →vaso-D; Tx: angina, CN poisoning(Sodium Nitrite forms methemoglobin) Tolerance develops quickly, Monday disease in explosive manufacturers
-Nitroglycerin, Isosorbide dinitrate, Amyl nitrite (inhaled, euphoria)
279
Calcium channel blockers for angina
Calcium Channel Blockers – oral; mainly renal excretion
-Verapamil–strongest cardiac effects; ↓HR, (-)inotrope, depress SA/AV; SE:constipation, depress cardiac too much AV block and cardiac arrest, inh platelets and insulin secretion -Diltiazem (Cardizem) – in between Verapamil and Nifedipine; depress SA/AV node directly Dihydropyridines- “-dipines”
Strongest vasodilators-arterioles; reflex tachycardia
-Nifedipine (Procardia) – oral/topical; Amlodipine (Norvasc), Isradipine
280
Beta blockers for angina
Beta Blockers
↓cardiac workload →↓O2 demand; ↓HR →↑perfusion time; ↓vaso-C
-Propranolol (ß),Metoprolol(ß-1), Atenolol(ß-1)
281
PDE-5 Inhibitors for angina
```
Phosphodiesterase-5 Inhibitors - oral
Inh PDE5(& some PDE6) →↑cGMP; Tx: erectile dysfunction; SE: headache, flushing; CI: Nitrates -Sildenafil (Viagra) – ~60 min to axn; CYP3A4; CI: nitrates, α blockers; SE: visual
-Vardenafil (Levitra) – more selective for PDE5→↓visual SE; faster onset of axn
-Tadalafil (Cialis) – longest duration of axn; allows for crazy weekends in Vegas
```
282
Nitroglycerin
Nitrate/nitrite used for angina
283
Isosorbide dinitrate (Isordil)
Nitrate/nitrite used for angina
284
Isosorbide mononitrate (Ismo)
Nitrate/nitrite used for angina
285
Nifedipine (Procardia)
Dihydropyridine type Ca channel blocker used for angina
286
Sildenafil (Viagra)
PDE5 inhibitor
Used for angina (and other uses)
~60 min to axn; CYP3A4; CI: nitrates, α blockers; SE: visual
287
Vardenafil (Levitra)
PDE5 inhibitor
Used for angina (and other uses)
more selective for PDE5→↓visual SE; faster onset of axn
288
Tadalafil (Cialis)
PDE5 inhibitor
Used for angina (and other uses)
longest duration of axn; allows for crazy weekends in Vegas
289
Avanafil (Stendra)
PDE5 inhibitor
| Used for angina (and other uses)
290
Ranolazine (Ranexa)
Treatment for angina
| oral; Inh. PFox, inh. Late Na current; ↓LV wall stiffness; Tx: chronic stable (not 1st line); SE: CYP3A4, teratogenic
291
Bosentan
Treatment for angina
| oral; endothelin receptor antagonist; only use in severe pulmonary HTN
292
Erythromycin
Macrolide–liver elim., good for kideny failure, not good for UTI's, protein synth inhibitor
reversibly binds 50S – inh translocation steps; alternative for penicillin allergy and when kidney failure; SAFE; spectrum similar to Pen G (gram +; (-) is resistant); Tx erysipelas due to GAS, pneumonia due to M. pneumoniae, chlamydia, and Legionnaire’s disease, also for Syphilis(those allergic to Pen G), can penetrate prostatic fluid; acid-sensitive – must be enteric-coated; inh. CYP3A4; antagonism w/ chloramphenicol(same binding site); no CNS; SE: GI disturbances, DIARRHEA, elevated hepatic enzymes, cholestatic jaundice, ototoxicity, may prolong QT, torsades; Resistance: is due to a Methylase(modify binding site); active pump or esterases & 50S mutation
293
Clarithromycin (Biaxin)
Macrolide–liver elim., good for kideny failure, not good for UTI's, protein synth inhibitor
similar mechanism; penetrates lung and macrophages: tx MAC(in immunocompromised), H. pylori-associated duodenal ulcers, community-acquired pneumonia (CAP)
294
Azithromycin (Zithromax)
Macrolide–liver elim., good for kideny failure, not good for UTI's, protein synth inhibitor
similar mechanism; dosed once daily; DOC for Legionnaires; effective against chlamydia and gonorrhea(ceftriaxone is DOC), pediatric otitis media, pharyngitis, and MAC prophylaxis; less effect on CYP3A4(NOT metabolized by P450 system; but still excreted in bile) and fewest overall SE/interactions
295
Telithromycin (Ketek)
Ketolides (altered Macrolide for the resistant organisms)
- Telithromycin(oral) – binds 50S; broad spectrum; tx respiratory pathogens, intracellular and atypical bacteria(for erythro/PCN resistant); SE serious hepatotoxicity
296
Clindamycin (Cleocin)
Protein synth inhibitor
(oral)binds to 50S; primarily in Tx of anaerobic bacteria infections – Bacteroides fragilis; effective w/ pyrimethamine(inh DHF reductase) in tx toxoplasmic encephalitis in patients w/ AIDS, Tx Osteomyelitis(b/c Staph causes it); SE well known cause of pseudomembranous colitis
297
Dalfopristin; Quinupristin (Synercid)
Streptogramins
(IV)– irreversibly blocks ribosome function 50S; tx vancomycin-resistant Enterococcus faecium –not faecalis (VRE); inh. CYP3A4; CI: breast-feeding, kids, prego’s, etc
298
Linezolid (Zyvox)
Oxazolidinone
reversible, non-selective inhibitor of MAO; blks formation of 70s – binding 50s; effective only against aerobic gram +; bacteriostatic; oral bioavailability 100%; metabolized via non- enzymatic oxidation (no interactions); tx VRE, MRSA, bacterial pneumonia; SE superinfection CI: hypersensitivity, pheochromocytoma
299
Aminoglycosides
Protein synth inhibitor
they bind irreversibly 30S and inhibiting initiation complex, blocking translation, and incorporating the wrong AA – Require Oxygen dependent active transport. Concentration dependent killing – Bactericidal(time dependent w/ PAE = 1 time daily); horrible oral absorption and CSF penetration; inh. gram – bacilli (AEROBIC coverage only); effective particularly against Pseudomonas aeruginosa; also indicated if suspicion of sepsis; SE ototoxicity, nephrotoxicity, NMJ inhibition (serious toxicity – tx w/ Ca++ gluconate or neostigmine); Used ONLY to tx severe systemic infections; renal excretion
300
Gentamicin
Aminoglycoside
(IV) topical application for tx burns and wounds; bactericidal in vitro against 95% S. aureus; DOC tularemia, w/ penicillin to tx Pseudomonas; (monitor plasma levels)
301
Tobramycin
Aminoglycoside
| IV) tx of severe infections (monitor plasma levels
302
Amikacin (Amikin)
Aminoglycoside
| IV) gentamycin-resistant infections may respond to this instead (monitor plasma levels
303
Streptomycin
Aminoglycoside
(IV) tx tularemia, bubonic plague (w/ doxycycline), Brucella, TB (second line), endocarditis(in combo – due to staph, strep, or enterococcus)
304
Spectinomycin
Aminoglycoside
| (off market) – tx uncomplicated gonorrhea in patients who are allergic to ceftriaxone,
305
Neomycin
Aminoglycoside
(topical); tx hepatic encephalopathy(NH4+ due to GI bacteria); prep for colon surgery- suppresses aerobic flora SE: severe hepatotoxicity if injected, contact dermititis
306
Paromomycin
Aminoglycoside
| (IV) tx intestinal amebiasis, Cryptosporidium parvum infections
307
Chloramphenicol
reversibly binds 50S (*anaerobes*); bacteriostatic; oral; 100% oral absorption, CNS penetration; not effective against E. histolytic or pseudomonas; resistance due to bacterial acetyl transferase; distributed widely (including CNS & eyes); second line Tx typhoid fever (bactrim first), meningitis(very effective; DOC is PCN), Rickettsia/brucellosis/RMSF(DOC is Doxycycline), topical tx eye infections, Infections from Gram(-) organisms; inh CYP450 - ↑ effect warfarin/phenobarbital/phenytoin, ↓ effect penicillin – metabolized in liver(90%) conjugated with glucoronic acid; SE: gray baby syndrome(inh mito.), deadly aplastic anemia(genetic) and bone marrow depression(does dependent-reversible – by binding the mitochondria 70S ribosomes)
308
Tetracyclines general
(oral) G(+ &-) and many of the big tough micro boys; tx H. pylori w/ metronidazole + bismuth; tx M. pneumonia, chlamydia, Lyme Disease(also ampicillin), Vibrio cholera, plague (w/ streptomycin), Brucella (w/ aminoglycoside), RMSF; bind specifically to 30S – blking access of the amino acyl-tRNA to the mRNA-ribosome complex; bacteriostatic; distribution wide except CNS and joints; aluminum and calcium salts may greatly inhibit intestinal absorption; SE: deposits in bone and teeth(like to go where Ca+ is), overgrowth of resistant flora(candida – like the inhaled corticosteroids); CI: pregnancy and children
309
Tetracycline
Broad spectrum inhibitor of protein synthesis
| short acting SE: skin eruption w/ sunlight
310
Demeclocycline
Tetracycline
| intermediate acting; SE: inh. ADH and skin eruption after sunlight
311
Doxycycline
Tetracycline
| (oral, IV) long acting – less intraxn w/ cations SE: skin eruption w/ sunlight
312
Minocycline
Tetracycline
| (oral, IV) long acting; ototoxicity – less intraxn w/ cations; 100% absorption on empty stomach
313
Tigecycline
Glycylcycline
(IV) derivative of minocycline; binds 30S; bacteriostatic; Tx: MRSA, MRSE, PRSP, VRE; biliary excretion; SE: same as tetracyclines
314
Nitrofurantoin (Furadantin)
UTI drug
broad spectrum; Good for E. coli, S. pyogenes, Citrobacter, Klebsiella, enterobacter; no proteus and pseudomonas coverage; > effect in acidic urine; SE: brown urine, methemoglobinemia, hemolysis, interstitial pulmonary fibrosis, severe polyneuropathies
315
Methenamine Mandelate (Mandelamine)
UTI Drug
decomposes to formaldehyde in the urine and binds amino groups; bactericidal; mandelate acidifies urine; mainly effective against E. coli; resistance does not develop; non-toxic
316
TMP-SMX for UTI
SE: thrombocytopenia due to folate metabolism interference; DOC for UTI’s
317
Treatments for UTI
Nitrofurantoin, methenamine mandelate, nalidixic acid, TMPSMX,, cephalosporines, gentamicin, tobramycin, amikacin, ampicillin, amoxicillin, some fluoroquinolones
318
DOC for listeria
Ampicillin
319
Fluoroquinolone MOA
enter thru porin channels, inh. DNA gyrase!(topoisomerase II – which inh the resealing of nicked DNA = cleavage of DNA(Gram -); and topoisomerase IV – needed for cell division(Gram +);bactericidal
320
Ciprofolxacin
2nd Gen. Fluoroquinolone
oral; broad spectrum bactericidal; highly active in vitro, especially against Pseudomonas aeruginosa and MRSA; less effective against gram +, anaerobes, and horrible CNS penetration, poor Strep pneumo coverage; DOC prophylaxis of inhalational anthrax; tx Shigella, soft tissue infections; SE: transient ↑ LFTs, tendon rupture, and QT prolongation, seizures in other fluoroquinolones and not cipro.
321
Norfloxacin
1st Gen. Fluoroquinolone
322
Ofloxacin
2nd Gen. Fluoroquinolone
323
Moxifloxacin (Avelox)
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3rd Gen. Fluoroquinolone
IDEAL - oral once-a-day; broad spectrum; better activity against penicillin- susceptible and –resistant pneumococci (Strep pneumo) (better gram +), better anaerobic coverage, better CNS penetration; tx CAP; SE: should be avoided in patients with long QT/patients receiving class IA (quinidine, procainamide, disopyramide) or III antiarrhythmics (amiodarone, sotalol, etc.)
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324
Gatifloxacin (Zymar)
3rd Gen. Fluoroquinolone
| topical for eye infections; off the market in 2006 due to SE: five-assed monkey
325
Metronidazole
DOC E. histolytica, G. lamblia, T. vaginalis, also for tx B. fragilis, C. difficile, & Gardnerella; SE: GI irritation, metallic taste, disulfiram-like(avoid EtOH), red urine
326
What are the first line TB drugs?
Isoniazid, Rifampin, Ethambutol, Pyrzinamide
| Rifabutin, Streptomycin
327
What are the second line TB drugs?
Aminosalicylic acid, Ethionamide, Rifapentine, Capreomycin, Clofazimine, Ciprofloxacin, Levofloxacin, Ofloxacin, Kanamycin
328
Isoniazid
TB drug 1st line
(oral)#1 stunna prophylaxis; oral; inh mycolic acid(gets intracellular) –bactericidal in rapidly dividing organisms; always given in combo w/ at least one other antiTB drug; rapid(inuits, Natives Amer) vs slow(blacks/whites) metabolizers; SE: CNS stimulation, peripheral neuropathy(due to B6 def), liver damage, hemolysis (G6PD deficiency) – INH and Rifampin given together
329
Ethambutol
TB drug 1st line
nh arabinosyl transferase; bacteriostatic; given w/ at least one other antiTB drug; renal excretion; good for MDR TB; SE: optic neuritis (decrease of visual acuityand loss of red-green perception)– not used in kids –last resort(given w/ vision tests; reversible if early detection)
330
Rifampin
```
TB drug 1st line
broad spectrum(G + and -) and all mycobaterium; inh. DNA-dependent RNA polymerase; bactericidal; activity approaches that of INH; effective against leprosy; SE: orange secretions(urine, sweat, tears), induces p450(not in HIV+ pts – switch w/ Rifabutin), decreases effectivenss of birth control
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331
Pyrazinamide
TB drug 1st line
| bactericidal; SE: hepatic injury
332
Streptomycin and TB
2nd line TB drug
| ront-line durg, but may be dropped down to second line; can’t affect intracellularly
333
Ethionamide
2nd line TB drug
| oral) neurotoxic(peripheral neuropathies – B6 def
334
Capreomycin
2nd line TB drug
| (IM) nephrotoxic and ototoxicity
335
Rifabutin
2nd line TB drug
(oral) front line in HIV+; taking protesase inh (can by prophylaxis in AIDS pt); less inducer of P450 ; urine discoloration, thrombocytopenia, polymyalgia
336
Drugs used in leprosy
Triple drug regimen for 6-24 months
Dapsone
Rifampin
Clofazamine
337
Dapsone
(oral) DOC leprosy and for P. jiroveci– start w/ low dose and increase over time; PABA antagonist; SE: methemoglobinemia, hemolysis(in G6PD def pt), peripheral neuropathy, nasal obstruction(will resolve) and cause erythema nodosum leprosum(ENL)
338
Clofazamine
Treatment for leprosy
binds preferentially to mycobacterial DNA(high GC content in mycobacterium); SE: crystalline deposits(red-brown skin discolor), hepatotoxic (No ENL)
339
Thalidomide
DOC erythema nodosum leprosum, tx HIV wasting syndrome; reduces levels of TNF-α; oral; pregnancy Category X
