Pharmacology Period 2

Front 1

Blocks inactive NaV.
For generalized tonic clonic seizures.
Not a central depressant.
Reduces spread by targeting excessively active regions.
Gingival hyperplasia is most common side effect.

Back 1

Phenytoin

Front 2

Blocks inactive NaV.
For generalized tonic clonic seizures and post herpetic neuralgia
Side effects include drowsiness, renal and hepatic, blurred vision.

Back 2

Carbamazepine

Front 3

GABA-mimetic.
For generalized tonic clonic seizures.
Currently not used much in favor of valproate.
Non-slsective CNS depressant.
Limits seizure spread, elevates spread, preventing recurrence of febrile-induced seizures.

Back 3

Phenobarbital (barbituate)

Front 4

GABA-mimetic.
Used to interrupt Status Epilepticus.

Back 4

Diazepam (benzodiazepine)

Front 5

Blocks rapidly inactivating T-type Ca++ channels.
For generalized absence seizures primarily, also for myoclonic seizures.
Side effects include GI distress, drowiness, and may cause seizures in pts with major motor epilepsy.

Back 5

Ethosuximide

Front 6

Block NaV. Some T-type Ca++ channels and GABA uptake also blocked.
For generalized absence and generalized tonic clonic.
Few CNS side effects. Good drug!

Back 6

Valproic Acid (Valproate)

Front 7

Blocks CaV and maybe NaV.
Excellent in neuropathic pain and low-level disorders.
Fewer side effects than most antiepileptics.

Back 7

Gabapentin
(Structural analog of GABA, but not a GABA agonist)

Front 8

Strongly blocks NaV
For complex partial seizures.
Can be used as an adjuvant.

Back 8

Lamotrogine

Front 9

Glycine antagonists at NMDA receptors.
Possibly blocks NaV.
For generalized tonic cloin and partial seizures.

Back 9

Felbamate

Front 10

Inhibits GABA uptake in to neurons.
For partial seizures.

Back 10

Tiagabine

Front 11

Blocks NaV.
Enhances efficacy of GABA, blocks AMPA.
For patial seizures.

Back 11

Topirmate

Front 12

Mechanism of action unknown.
For long term treatment of anxiety, especially in the elderly.
Non-sedative.

Back 12

Buspirone

Front 13

For insomnia.
Short half-life.

Back 13

Triazolam

Front 14

For generalized anxiety disorder and panic/phobia disorder.
Use a low dose for daytime anxiety.
Medium half life.

Back 14

Alprazolam

Front 15

For generalized anxiety disorder, panic/phobia disorders, and insomnia.
Use a low dose for daytime anxiety.
Use a high dose for insomnia.
Long half life.

Back 15

Dizepam

Front 16

Reversible depression of all excitable tissue, though CNS is most sensitive.
Small doses are hyperalgesic.
Short acting.
Side effects are hangover (extended CNS depression), paradoxical excitement, hepatic enzymatic drug interactions, withdrawl is bad.

Back 16

Secobarbital

Front 17

Acts on benzodiazepine site on GABA receptor, but not a benzodiazepine.
For insomnia. Cannot relive anxiety at high doses.
Tolerance not much of an issues.

Back 17

Zolpidem

Front 18

Used to treat chronic alcoholism.
Inactivates aldehyde dehydrogenase, allowing acetylaldehyde to accumulate.

Back 18

Disulfiram

Front 19

Used for fever, as a vehicle, skin disinfectant, prevent decubitus ulcers.
Antidote to methanol poisoning.
Enhances GABA, inhibits NMDA, enhances 5HT3

Back 19

Ethanol

Front 20

5-HT B/D agonist.
For acute migraines.
Potent vasoconstrictor of vessel SMC.
Reduces secondary pain flow to thalamus.
Side effects are minor, but contraindicated in pts with CAD.

Back 20

Sumatriptan

Front 21

Non-selective for 5HT, Da, and alpha adrenergic receptors. Theraputic effects likely from 5-HT1 receptors.
For acute treatment of frequent moderate migraines or infrequent severe migraines.
Side effects are nausea and vomiting in 10% of pts, may exacerbate angina, not for the pregnant.

Back 21

Ergotamine

Front 22

Serotonergic antagonist.
For migraine prophylaxis.
Side effects - can cause retroperitoneal fibrosis that requires discontinuation of treatment for 1 month every 6 months.

Back 22

Methylsergide

Front 23

Possible AD prophylaxis. 2 year treatment reduced AD risk by 55% in elderly who took drugs before, had no prior AD symptoms.

Back 23

NSAIDs

Front 24

Possible AD prophylaxis.
Reduces AD risk by 79% in one study.

Back 24

Statins
Hypercholesterolemia correlates with increased AD incidence in later life.

Front 25

Possible AD prophylaxis.
Thought to reduce AD by reducing hypertension.

Back 25

Anti-hypertensives.

Front 26

A butrylcholinesterase inhibitor.
Was the prototype AD drug.
Non-selective PNS and CNS inhibitor.
Short half-life, must be given 4 times daily.
Side effects are cholinergic in nature.
Causes direct hepatic damage.

Back 26

Tacrine

Front 27

CNS-selective acetylcholinesterase inhibitor.
Drug of choice for AD pts NOT ON multi-drug regimens.
Long half life - once daily.
Side effects are cholinergic in nautre.
No direct hepatic damage.
Metabolized by a cytochrome P450 isoensyme. Risk of adverse drug interactions high.

Back 27

Donepezil

Front 28

CNS-selective acetylcholinesterase inhibitor.
Drug of choice for AD PTS ON multi-drug regimens.
Inhibitor medium length - take 2 daily.
Side effects are cholinergic.
Metabolized by cholinesterases so reduced risk of drug interactions.
Reduced hepatotoxicity.

Back 28

Rivastigmine

Front 29

Non-selective CNS and PNS acetylcholinesterase inhibitor.
Uncertain clinical use, potentiates nicotinic receptor, which is one possible use.
Considered an AD drug.
No direct hepatic toxicity.

Back 29

Galantamine

Front 30

NMDA receptor antagonist.
Can slow deterioration in AD alone and with Donepezil.
Just FDA approved in US.

Back 30

Memantine

Front 31

Blocks NE reuptake in CNS and peripherally.
For mood elevation in special cases. Beware side effects.
Side effects - orthostatic hypotension, tachycardia, arrhythmia, sedation, anticholinergic effects, weight gain.
Suicide can be achieved by taking a weeks supply.

Back 31

Nortriptyline

Front 32

Blocks degradation of NE, DA, 5-HT, other amines.
For atypical depression and major depression when other drugs are not effective or appropiate.
Side effects - hepatotoxicity, potentiates sympathomimetic amines, hyperreflexia, and convulsions.
Tyramine reaction occurs - avoid wine and cheese.

Back 32

Phenelzine

Front 33

Selectively inhibits 5-HT reuptake.
For mood elevation in 1-3 weeks.
Also for OCD, atypical depression, panic disorder, bulemia, with other drugs for bipolar.
Side effects - Sexual dysfunction, slow onset, 10% get naseua and diarrhea, suicidal thinking in adolescents, contraindicated in anorexics.

Back 33

Fluoxetine

Front 34

Inhibits reuptake of NE and 5-HT
Fewer side effects than tricyclics.
Similar side effect profile to SSRIs.
Short half life.

Back 34

Venlafaxine

Front 35

5-HT reuptake inhibitor. Also a partial agonist at 5-HT1aR.
Used for depression with insomnia, anxiety, and agitation.
Side effects - marked sedation, dizziness, hypotension, naseua.

Back 35

Trazodone

Front 36

5-HT reuptake inhibitor that is also a 5-HT2 antagonist.
Produces non-sedating mood elevation.
For depressed people with fatigue.

Back 36

Nefazodone

Front 37

Inhibits DA and NE reuptake.
For depression, especailly with psychomotor retardation.
For treatment of nicotine addiction.
Low side effects, include nervousness and insomnia.

Back 37

Bupropion

Front 38

Alpha 2 antagonist and 5-HT 2 + 3 receptor antagonist.
Mood elevation but has sedative and anxiolytic effects.
Side effects similar to TCAs.

Back 38

Mirtazapine

Front 39

For treatment of acute mania (with benzodiazepine), manic phases of manic-depressive illness, mood swings of manic-depressive prone pts, anti-depressant effect in some.
Side effects - fatigue, muscular weakness, slurred speech, ataxia, thirst, urination.
Tolerance eventually develops to many side effects.

Back 39

Lithium

Front 40

Stimulates hyptocretin/orexin neurons, predominantely in hypothalamus.
For narcolepsy, shift-work sleep disorder, possibly useful for ADHD in future.
Low abuse liability.
Fewer classicla stimulant side effects

Back 40

Modafinil

Front 41

Selective NE reuptake inhibitor.
For ADHD in children and 1st and only drug for ADD in adults.
Not a stimulant.
Side effects - hepatoxicity, decreased appetite, insomnia, sexual issues.

Back 41

Atomoxetine

Front 42

Antagonize adenosine receptors, levels of which may signal fatigue.
For bronchial asthmas - relax smooth muscle, with asprin for headaches, with ergots for migraine - improve their absorption.
Side effects - nervousness, insomnia, excessive respiratory stimulation, tolerance, but modest withdrawl.

Back 42

Caffeine

Front 43

Evoke release and inhibit reuptake of NE and 5-HT. Also have effects on DA.
First-line drug in ADHD. Also used in nacrolepsy and previously used in obesity.
Competes with NE for reuptake transporter and VMAT.
Causes wakefulness, tremor, dilated pupils.

Back 43

Methylphenidate

Front 44

Blocks reuptake of biogenic amines, especially dopamine.
Principle use is as anesthetic in upper respiratory tract. Vasoconstricts and reduces secretions.
Causes wakefulness, tremor, dilated pupils.

Back 44

Cocaine

Front 45

Evoke release and inhibit reuptake of NE and 5-HT. Also have effects on DA.
Used for narcolepsy. Can be used for ADHD, but is not first-line.
Competes with NE for reuptake transporter and VMAT.
Causes wakefulness, tremor, dilated pupils.

Back 45

Dextroamphetamine

Front 46

Causes pleasure (dopamine), appetite supression (norepinephrine), cognitive enhancement (acetylcholine), memory (vasopressin), mood modultion (serotonin), anxiety reduction (beta-endorphin)

Back 46

Nicotine

Front 47

Blocks NE reuptake. Effective in aiding smoking cessation. Has some side effects.

Back 47

Nortriptyline

Front 48

Blocks DA and NE reuptake. Effective in aiding smoking cessation. Has few side effects.

Back 48

Bupropion

Front 49

CB1 receptor antagonist.
Helps stop you from smoking weed. And has some use in getting you off the coke, morphine, booze, and food.

Back 49

Rimonabant

Front 50

Precursor to DA.
Crosses BBB to enter brain and is metabolized to DA.
Used to treat parkinsonism.
Only 5% actually gets in brain because 95% is converted to DA in periphery and later to NE.
Causes peripheral DA and NE toxicity - orthostatic hypertension, nasea, dyskinesia, psychosis (dopamine in limbic and corticol areas).

Back 50

Levodopa

Front 51

Has been tried to be given to treat parkinsonism.
Given orally will make you vomit.
Will not cross BBB and causes vomiting when in periphery.

Back 51

Dopamine

Front 52

Peripheral decarboxylase inhibitor.
Used with another drug to treat parkinsonism.
Circumvents peripheral DA toxicity and blocks Vitamin B effect.

Back 52

Carbidopa

Front 53

Best treatment for PD.
Increases life expectancy with minimal side effects.
No resistance develops.
Some peripheral side effects are present - orthostatic HTN, nausea, vomiting, dyskinesis, pyschiatric effects.

Back 53

Sinemet (Levodopa and Carbidopa)

Front 54

Blocks action of ACh.
Early drug used to treat PD, enhance motion by stimulating caudate.
Side effects - especially in elderly - low theraputic index, sedation, delerium, tachycardia, anti-salivation, anti-lacrimation, anti-urination, anti-defication (SLUD).

Back 54

Trihexyphenidyl

Front 55

Peripheral COMT inhibitors.
COMT is the enzyme that breaks down L-DOPA. Decreases L-DOPA elimination.
Used to extend Sinemet duration of action and decrease it's on/off and weaning off effects. One of these drugs can cause liver failure - which one?

Back 55

Tolcapone (liver failure) and Entacapone.

Front 56

D2 agonist and partial D1 agonist/antagonist.
Used to aid Sinemet in late-stage PD, used alone in early PD, can also treat associated hyperprolactinemia (pituitary D2 receptros block prolactin secretion)

Back 56

Bromocriptine

Front 57

Dopamine D1/D2 agonist.
Used to aid Sinemet in late-stage PD and used along in early PD.
Incidence of side effects lower than with D2 agonists.
Possibly aleviates on/off phenomenon, due to prolonged action.
Moderate half-life.

Back 57

Pergolide

Front 58

Enhances DA release of Substantia Nigra, blocks glutamate.
Used to aid Sinemet in late-stage PD and can be used alone in early stage.
Side effects similar to anti-cholinergics.
Started as anti-viral.

Back 58

Amantadine

Front 59

Inhibits metabolism of brain DA to DOPAC via MAO-B inhibition.
Provides mild symptomatic relief, expensive.
Has uncertain neuroprotective effect.

Back 59

Selegiline

Front 60

Dopamine D3>D2 agonist.
Used to aid Sinemet in late-stage PD and can be used alone in early PD.
Can also be used with restless leg syndrome.
Side effects include sleep attacks, hallucination, dyskinesia, nausea. Somewhat more effective than bromocyptine.
No ergoline-like side effects.

Back 60

Pramipexole and Ropinirole

Front 61

Powerful D1/D2 agonist.
Used to rescue PD patients rapidly from the off-state.
Administed IV, sublingual, rectally, intranasal, pen-injection.

Back 61

Apomorphine

Front 62

Strong D2 receptor antagonist.
Used to treat psychosis.
High sedative, moderate hypotensive, low motor side-effects.
A phenothiazine with high anti-cholingergic and anti-adrenergic properties so pseudoparkonism side effect is not present.
Can cause Neuroleptic Malignant Syndrom (NMS).

Back 62

Thioridazine

Front 63

Strong D2 receptor antagonist.
Used to treat psychosis.
Low sedative, low hypotensive, high motor side-effects.
High pseudoparkinsonism and tardative dyskinesia motor side effects.
A phenothiazine, but low anticholinergic properties so

Back 63

Fluphenazine

Front 64

Strong D2 receptor antagonist.
Low sedative, low hypotensive, high motor-side effects.
High pseudoparkinsonism and tardative dyskinesia motor side effects.
A butyrphenone, so more D2 selective.

Back 64

Haloperidol

Front 65

Strong D2 and strong 5HT2 receptor antagonist.
Used to treat psychosis.

Can possibly increase anxiety and depression.

Back 65

Risperidone

Front 66

Strong 5-HT2 antagonist and weak D2 antagonist.
Atypical anti-psychotic drug of choice of the moment.
Strong anti-cholinergic, so few to no motor side-effects.
Causes potentially fatal agranulocytosis in up to 3% of patients - so monitor blood.
May partly relieve tardive dyskinesia.

Back 66

Clozapine

Front 67

Strong 5-HT2 and weak D2 antagonist.
Used to treat psychosis.
Low to none motor side effects.
Possible new best atypical anti-psychotic.
No risk of aganulocytosis!

Back 67

Olanzapine

Front 68

Strong 5-HT2 and weak D2 antagonist.
Used to treat psychosis.
Low to none motor side effects.
Also used to alleviate dopaminergic treatment-induced psychosis/hallucinations in PD.

Back 68

Quetiapine

Front 69

Strong 5-HT2 and weak D2 antagonist.
Used to treat psychosis.
Low to none motor side-effects.
May not cause weight gain like other psychotics.
Side effect: Prolonged QT interval.

Back 69

Ziprasidone

Front 70

Mild presynaptic D2 agonist (reduced DA release from substantia nigra) and postsynaptic D2 antagonist (reduced DA effects on striatum).
Low to no motor side effects.
Milder action and inhibition of DA release which appears to prevent motor side effects and tardive dyskinesia.
May not cause weight gain like other psychotics.

Back 70

Aripiprazole

Front 71

Good analgesic, weak anesthetic.
Rapid uptake and elimination.
High MAC.
No odor, no metabolism, no hepatic toxicity.
Little cardiac or respiratory depression.
Can easily distend air spaces.

Back 71

Nitrous Oxide

Front 72

Effective anesthetic at low concentrations.
Causes hepatic necrosis.
Can result in a hepatitis in rare cases.
Little airway irritation.
Slow uptake and elimination.

Back 72

Halothane

Front 73

Good anesthetic and muscle relaxant.
Pungent odor - bronchoiritating with laryngospasm.
No renal, low metabolism with only reported liver toxicity.
Stable cardiac rhythm and rate.
Vasodilates and reduces systemic vascular resistance.

Back 73

Isoflurane

Front 74

Good anesthetic.
Rapid uptake and elimination.
Generally used for matentience of anesthesia.
Minimal systemic and side effects.
High incidence of coughing and laryngospasm, raises airway resistance.
Protective airway responses come back quickly and general recovery is quick after discontinuation.

Back 74

Desflurane

Front 75

Good anesthetic.
Rapid uptake and elimination.
Generally used for inductgion of anesthesia.
Minimal systemic and side effects.
No coughing or layngospasm, lowers airways resistance.
Strong vasodilation.
Rocovery longer and expensive.

Back 75

Sevoflurane

Front 76

Anesthetic similar to isoflurane with renal toxicity.
Smells bad like isoflurane.

Back 76

Enflurane

Front 77

Used for normal amnesia and normal outpatient anestesia.
No analgesia.
Unpredictable hypnosis.
Strong amnesia.
Enhances GABA function. Unlike others, can be reversed.

Back 77

Midazolam

Front 78

Used for a cerebral protective operation because it decreases cerebral metabolic rate for oxygen.
Low pain on injection compared to other drug in class.
Used for low cost induction.
No analgesia. (Or possibly hypo-algesia in low doses).
Strong hypnosis.
Weak amnesia.
Enhances GABA function.
Cardiac depressant.

Back 78

Thiopental

Front 79

Can be used for a cerebral protective operation because it decreases cerebral metabolic rate for oxygen. Slightly worse for perfusion pressure and ICP than other agent used for same thing.
No analgesia.
Strong hypnosis.
Moderate amnesia.
Enhances GABA function.
Painful on injection.
Minimal hangover and nice anti-emetic effect.

Back 79

Propofol

Front 80

Used for normal analgesia when lower doses are needed.
Also used to help lessen pain peri-operatively and chronic pain.
Used in low blood pressure emergencies and for long procedures.
Strong analgesia.
Moderate hypnosis with hallucinations in some groups.
Moderate amnesia.
Raises systemic blood pressure.
Bad side effect - increases ICP.
Stable with a context sensitive half life.
Competivie inhibitor of NMDA.
Not painful on injection.
Only drug safe with porphyria.

Back 80

Ketamine

Front 81

Used for brief procedures like cardioversion and electroconvulsive therapy.
Cadiac depressant.
Enhances GABA function.
No analgesia.
Strong hypnosis.
Weak amnesia.

Back 81

Methohexital

Front 82

Used on patients with cardiac disease because its only anesthetic that has no effect on Cardiac system and also used for brief procedures like cardioversion and electroconvulsive therapy.
Only IV anesthetic that does not cause histamine release.
Enhances GABA function.
No analgesia.
Strong hypnosis.
Weak amnesia.
Blocks normal stress-induced cortisol and cannot be used in the ICU when pts are under high stress.
Painful on injection.

Back 82

Etomidate

Front 83

Used as sedative in ICU.
Also used as an adjuvant.
Also used to potentiate anesthesia, assist with intubation, and as a general anesthetic when you don't need deep levels (ie patient can talk).
Alpha 2 agonist.
Problems - slow onset, hypotension, bradycardia, pain on injection.

Back 83

Dexmedetomidine

Front 84

Function like Midazolam, but has an aqueous base, so more pain on injection so not used. Can be reversed.

Back 84

Diazepam

Front 85

Amide class LA.
Associated with nerve toxicity when used as a nerve block and has ability to difuse through bone.

Back 85

Articaine

Front 86

Amide class LA.
Often used for post-op analgesia (Marcaine block).
Extensive protein binding, so long acting but slow onset.
As 0.5% solution with epi.

Back 86

Buprivicaine

Front 87

Amide class LA.
1.5% with epi.
Long acting due to high protein binding.
Greater lipid solubility, so more potent.
Onset 3-5 min, length 5-10 hours.

Back 87

Etidocaine

Front 88

Amide class LA.
Used commonly world-wide.
Very safe.
2% concentration with vasoconstrictor.
Can use pupal anesthesia test for pain.
Use with epinephrine.
Can have allergy to catecholamine give with it, but not the druf itself.
Can have complications with liver or renal disease.

Back 88

Lidocaine

Front 89

Amide class LA.
Used as 3% solution without vasoconstrictor.
Inherently a mild vasoconstrictor (safe to inject at areas with end organ circulation)
Good for cardiac pts where you want to avoid catecholamines.
Quick onset (30 sec to 4 min) and short duration (half hour).
Works for 60 min as a block.
Sulfite free.

As a 2% concentration with levonordefrin (vasoconstrictor), can use for 1 to 5.5 hours.

Back 89

Mepivacaine

Front 90

Amide class LA.
High PKA so slow onset.

Back 90

Prilocaine

Front 91

Ester class LA.
Used in ENT cases.

Back 91

Cocaine

Front 92

Ester class LA.
Most commonly used in this class.

Back 92

Benzocaine

Front 93

Ester class LA.
Topical

Back 93

Butacaine.

Front 94

Potent vasoconstrictor.
Also used in dentristy.
Cardiac patients should receive less than max full dose.

Back 94

Epinephrine

Front 95

Mildly potent vasoconstrictor.
Acts on alpha sites.
Cardiac patients should receive less than max full dose.

Back 95

Levonordefrin