Medical Pharmacology Test #5

Front 1

Metabotropic Receptors

Back 1

alpha-adrenergic
beta-adrenergic
5HT (except 3)
Dopamine
Muscarinic ACh
Histamine/Neuropeptide
GabaB
Glutamate

Front 2

Ionotropic Receptors

Back 2

Depolarizers:
AMPA (Na)
Kainite (Na)
NMDA (Ca,Na) Glutamate
Nicotinic ACh (Na, Ca)
5HT3 (Na)
Hyperpolarizers
GabaA (Cl)
Glycine (Cl)

Front 3

Catecholamines General

Back 3

-Dopa, Norepi, Epi
-TH is rate limiting step (need tyrosine)
-terminated by MAO, COMT, reuptake (80%)

Front 4

Dopamine

Back 4

-D1, D5: increase cAMP
-D2,3,4: decrease Ca conductance, activate K channels
Metabolism:
-DA to DOPAC via MAO
-DOPAC to HVA via COMT

Front 5

Dopamine Tracts

Back 5

-Mesocortical/limbic: behavior, emotion
-Nigrostriatal: motor function
-Tuberoinfundibular: inhibits PRL

Front 6

Norepi/Epi

Back 6

-A1: increase Ip3, DAG
-A2: inhibit cAMP (presyna)
-B1: increase cAMP (heart, brain)
- anxiety, mood, arousal, memory, dreaming
Metabolism: COMT to MHPG (postsynap), VMA (mito)

Front 7

Indolamine (Serotonin, 5Ht)

Back 7

- made from Tryptophan
- terminated by reuptake, MAO-A breakdown
- hallucinations, mood, sensory perceptions, sleep, appetite, pain
Metabolism: to 5H1AA by MAO

Front 8

Acetylcholine

Back 8

- terminated by AcHe in cleft
- M1,3,5: excitatory (dec K)
- M2,4: inhibitory (inc K)
- Nic: excitatory (in Ca, Na)
- memory, motor, sensory

Front 9

Excitatory Amino Acids

Back 9

Glutamate, Aspartate
- NMDA receptor (Na, K, Ca)
- major excitatory trans of brain, spinal dorsal roots
- ketamine, PCP block NMDA (Glutamate antagonists)
- Zn, Mg block channel
- are excessively activated in stroke, ischemia, brain injury

Front 10

Inhibitory Amino Acids

Back 10

GABA, Glycine
- generally hyperpolarize via postsyn Cl channel (GabaA)
- GABA main one in brain (A: midbrain, cerebellum; B:CNS)
- GABA to SSA to Succinate (GabaT and SSADH)
- benzo, barb are allosteric activators
- BACLOFEN: GabaB agonist for spasticity

Front 11

Neuropeptides General

Back 11

- made in soma
- do NOT undergo presynaptic uptake
- are cotransmitters

Front 12

Substance P

Back 12

- Dorsal root ganglia, sensory transmitter of PNS
- transmits pain, behavioral effects
- NK receptors (Nk1 activated Phospho C)

Front 13

Opioids

Back 13

- Enkephalins from proenkeph (delta > mu)
- Endorphins from POMC (mu and delta)
- Dynorphins from prodyn (kappa)
- nociceptive response, all are Gi activating (inhibit cAMP)

Front 14

Leptin

Back 14

- peptide involved in regulating body weight
- receptors in hypothalamus
- increased levels, decreased body weight

Front 15

Orexin

Back 15

- stimulates body appetite
- stimulates drug seeking behavior
- potential role in narcolepsy

Front 16

Histamine

Back 16

- sedative effects via CNS receptors (H1 in hypothalamus)
- may modulate NMDA receptor action

Front 17

Purines

Back 17

- adenosine may be neurotransmitter
- Caffeine & antagonists are stimulants; agonists are depressants
- G proteins

Front 18

Nitric oxide

Back 18

- gas produces in nerve cells (iNOS, nNOS) and endothelial cells (eNOS)
- can diffuse (no vesicles)

Front 19

Benzodiazepines General

Back 19

- MOA: enhance binding to GABA-A, increase Cl entry, hyperpolarize and inhibit cell activity, increase channel opening (dose dep:anxio to sleep to anesthetic)
- Tx: anxiety, Etoh w/d, pania, isomnia, status epilepticus
- C/I: Antacids block, HM by p450 [no induction: oxi, hydroxy,glucon] (liver dis); respiratory; etoh; elderly
- S/E: anterograde amnesia, rebound insomnia, sedating, confusion; Xplacenta, milk; GI
- W/D syx: anxity, insomnia, seizures

Front 20

Long acting benzos

Back 20

Chlorazepate
Cloradiazepoxide
Diazepam (valium)
Flurazepam
Quazepam
Halazepam

Front 21

Intermediate benzos
* use in elderly

Back 21

Alprazolam (Xanax)
Estaxolam
Lorazepam (ativan)*
Temazepam (restoril)

Front 22

Short benzos
* use in elderly

Back 22

Oxazepam*
Triazolem (halcion)
Clonazepam (Klonopin)
Midazolam (Versed)

Front 23

Benzo precautions

Back 23

- Elderly: use short t1/2 (loraz, oxaze)
- Liver: potentiated (use loraz, oxaz)
- COPD: midazolem has extra respir effetcs
- aggrav. OSleepA
- additive with EtOH
- tolerance to hypnotic, MR effects

Front 24

Flumazenil

Back 24

BDZ competitive Agonist
- IV for OD
- may precipitate withdrawal

Front 25

Buspirone

Back 25

nonBDZ for GAD
- 5HT1a agonist (presynaptic autorecp)
- very slow onset, good for ppl with abuse probs b/c no depend or w/d
- no sed, anticonvuls or mr effects
- also good for elderly

Front 26

Meprobamate

Back 26

- propanediol
- unknown MOA (thalamus/limbic system)
- not as effective as BDZ
- can make porphyrias worse

Front 27

Propanolol

Back 27

- BBlocker for somatic anxiety syx
- stage fright

Front 28

Hydroxyzine

Back 28

- antihistamine
- causes sedation

Front 29

BDZs for sleep disorders

Back 29

- Flurezepam, Temazepam, Triazolam, Quazepam, Estazolam
-decrease sleep latency & awakenings
- increase stage 2, decrease 3/4 REM (# REM up, but time down)
- increase sleep time NET
- tolerance developes & REM rebound * except Temazepam

Front 30

Chloradiazepoxide

Back 30

Tx: anxiety, preanethesia, Etoh W/d
- rapid onset
- long duration
- DesmethCDP metabolite

Front 31

Diazepam

Back 31

Tx: all anxiety diorders -NO insomnia
- rapid onset
- long duration
- DesmethDZP met
- DIRECT muscle relaxant

Front 32

Triazolem

Back 32

Tx: insomnia, anxiety
- rapid onset
- ultrashort duration of action
- GET REBOUND INSOMNIA

Front 33

Alprazolam

Back 33

Tx: Anxiety, DOC for AGORAPHOBIA & PANIC
- rapid onset
- intermediate duration

Front 34

Lorazepam

Back 34

BDZ also used for seizures, antiemetic

Front 35

Zolpidem (Ambien)

Back 35

- NonBDZ for insomnia
- acts at BDZ receptors
- quick onset, selective hypnotic; PRESERVES normal sleep architecture
S/E: dizzy, HA, sleepy, Xr with ETOH

Front 36

Zaleplon

Back 36

- binds BDZ receptor
- rapid onset, short duration (can be dosed in middle of night)
- rebound insomnia possible

Front 37

Eszopicione (lunesta)

Back 37

- bdz like
- longer half and duration of action
- can be used long term

Front 38

Barbituates General

Back 38

- MOA: potentiate GABA, increase CL conductance, open channel for longer periods of time; inhibit glutamate (excitatory); mimic GABA at high doses
- Tx: sedative/hypnotic (kids), antagonist of stimulants, anticonvulsant, induce anesthesia
- decreases sleep 3/4/REM (tolerance devos)
- S/E: depress respire, INDUCE P450; X placenta, milk; additive with others; hyperalgesia
- C/i: porphyrias, preg, MAOis

Front 39

Long Acting Barbituates

Back 39

- Phenobarbital (anticonvulsant)
- Butabarbital

Front 40

Intermediate Barbituates

Back 40

- Amobarbital
- Butalbital
- Mephobarbital
- Pentobarbital
- Secobarbital

Front 41

Short Barbituates

Back 41

-Thiopental (induce anesthesia)
-Thioamylal
-Methohexital

Front 42

W/D or Abstience from Barbs

Back 42

- potentially life threatening
- GABA receps get down regulated
- intense AcH activity when stopped, little GABA - massive overexcitement
- life threatening seizures, arrythmias

Front 43

NonBarb Sedatives

Back 43

- Methyprylon, Glutethimide, Methaqualone, Ethchlorvynol
-CHLORAL HYDRATE (rapid, short duration, wide margin of safety, enhances ETOH - knock out drops)
- Antihistamines (diphenhydramine, doxylamine)
- Etoh

Front 44

Disulfram

Back 44

-Antabuse, inhibits aldehyde dehydro - so flush, tachy, hypervent, nausea, vomit with Etoh

Front 45

Naltrexone

Back 45

- opioid receptor antagonist (mu)
- reduces craving, blunt pleasure
- S/e nausea

Front 46

Acamprosate

Back 46

- analog of GABA
- decreases glutamate during ETOH w/d so helps prevent relapse

Front 47

Melatonin
(Ramelton is receptor agnoist)

Back 47

- made from tryptophan in pineal gland
- increases in evening, decreases am; thought to be related to diurnal rhythm maintenance

Front 48

Nacrolepsy Drugs

Back 48

- Methylphenidate (stimulant)
- sodium oxybate (GHB, stimulant)
- Modafinil (stimulant)

Front 49

DES

Back 49

- used to prevent premature birth
- transplacental CA: Clear cell vaginal cancer in daughters

Front 50

Thalidomide

Back 50

- used to control nausea/vomiting during pregnancy
- amelia, phocomeila in babies
- now used as immunosuppressant, chemo agent in myeloma and blood CAs

Front 51

Drugs to Avoid in Preggers

Back 51

-aspirin
-aminoglycosides
-antithyroid
-benzos
-chloramphenicol
- warfarin
- sulfonylureas hypogylcemics
- sulfonamides
-tetracyclines
- thiazides
- paroxetine (paxil)

Front 52

Drugs OK in Preg

Back 52

- PCNS, Acetaminophin
- heparin
- insulin
- iron, folic acid
- TMP/SMX
- topicals
- propylthiouracil
- metformin
- labetalol, methyldopa

Front 53

Halogenated Anesthetics

Back 53

-halothane, isoflurane, enflurane, sevoflurane, desflurane

(Nitrous is non halo)

Front 54

MAC

Back 54

-concentrater required to produce anesthesia in 50%
- affected by age, health, drug interactions
- NOT affected by gender, height, weight, duration, type of noxious stimultus
- induction dep on blood:gas partition coeff, vent rate, CO, alveolar pp

Front 55

Halothane

Back 55

- potent anesth., weak analgesic
- coadmin with NO, opiods or local
- pleasant odor
- S/E: CV, increased risk of arrhyth b/c sens to catechols
- dose dep bradycardia, drop in respire rate
- CAN CAUSE HEPATITIS (not in kids)

Front 56

Halothane + Succinylcholine

Back 56

-increased risk of malignant hyperthermia
- tx with DANTROLENE (cuts of Ca signaling)
(all halos + succ)

Front 57

Enflurane

Back 57

- rapid induce/recove
- less potent, pleasant odor
-S/E: some effects on heart, but not as bad as halo; dose dep respire depress; potentiated MRs
- CAN CAUSE SEIZURES
- Renal excretion, esp of F-, so caution in CRF pts

Front 58

Isoflurane

Back 58

- rapid induction, smooth recovery
- PUNGENT odor, so used for maint, not induction
- does NOT have CV effects
- S/E: dose dep respir dep, cns dep of SKM, very low organ toxic

Front 59

Desflurane

Back 59

- newer, very rapid induction/recovery
- S/E: dose dep drop of BP, RESPIRATORY IRRITANT (cough) so used in maintence, CNS dep of SKM

Front 60

Sevoflurane

Back 60

- new, rapid, odor not as pungent
- similar to desflurane in having good S/E profile
- REACTS with SODA lime in BREATHING APARTUS, so need spec equip
- Fl ions in met can be toxic in CRF pts

Front 61

Nitrous Oxide (N20)
[laughing gas]

Back 61

- potent analgesic, but weak anesthetic so combo for balance
- little effect on CV, AND allows for LOWER dose of halos in combo
- use 30% O2 with it
- can increase vol/pressure in middle ear, pneumothro, guts, lungs b/c replaces n2
- chronic use cases MEGALOBLASTIC ANEMIA

Front 62

Propofol

Back 62

- IV sed/hypno used to induction & main of anesth
- less hangover, better recover
- CV rep dep dose dep
- not analgesic
- outpatient procedures

Front 63

Etomidate

Back 63

- non barb sed hypno for induction of anesth
- miminmal CV effects
- DECREASE Blood to BRAIN - NEURO SURGERY
- not analgesic
- post op N/V common

Front 64

Thiopental
Methohexital
Thiamyl

Back 64

-sulfated ultrashort Barbs for induction/sed for anesth
- no analgesia, no MR
- potentiate GABA, increase duration of opening)
- may worsen shock, depress resp
- no antagonist for OD, induce P450
- C/I in porphyria

Front 65

Diazepam
Lorazepam
Midazolam

Back 65

-BDZ/CNS depressants used to reduce anxiety, induce sedation to facility anesthesia
- prevent convulsions, may depress respiration
- increase freq of GABA channel opening
[flumazenial is antagonist]

Front 66

Fentanyl
Morphine
Sulfenatanil

Back 66

-opioids for analgesia
- used in CV surg b/c preserve CO and contractility
- can CAUSE hypotension, resp dep, post op n/v
[naloxone is antagonist]

Front 67

Atropine
Scopolamine
Glycopyrrolate*

Back 67

-Anticholinergics used to combat secretions
-prevent vagal effects

Front 68

Neurolepthanesthesia

Back 68

- analgesia and sedation for surgery, but conscious to permit response to questions

Front 69

Droperiodol + Fentanyl

Anesthetic + Drop. + Fent.

Back 69

NeuroleptANALGESIA

NeuroleptANESTHESTIA

Front 70

Ketamine

Back 70

-related to PCP, blocks NMDA receptor
- dissociative anesthetic (no complete LOC)
- induction with profound analgesia
- delirium, hallucinations, irrational behavior in adults

Front 71

Stages of Anesthesia

Back 71

I: analgesia
II: Excitement
III: Surgical
IV: Medullary paralysis
(want to skip through II and not get to IV)

Front 72

Benzocaine
Procaine
Cocaine
Chloprocaine

Back 72

-Ester based local anesthetics
- metabolized by esterases, plasma
- bind to Na channel, reversibly inhibit axonal nerve conduction (aff for open channels, block increases with firing rate)
-Esters met to PABA so ALLERGY possible!

Front 73

Bupivacaine
Etidocaine
Lidocaine
Mepivaine
Prilocaine
Ropivicaine

Back 73

- Amide local anesth.
- metabolized in liver by amidases
- reversibly block Na channels (like esters)
- LESS likely to cause allergy

Front 74

Epinephrine
Phenylephrine

Back 74

- vasoconstrictors used to slow rate of absorp, decrease plasma con of locals
- do NOT use in end artery areas (fingers, toes, ears, nose, penis)

Front 75

Bupivacaine

Back 75

- used for epidural during labor/delivery (caudal space)

Front 76

Cocaine

Back 76

- only local that causes vasoconstriction, used topically in ENT surgery

Front 77

Procaine

Back 77

- 1st synthetic local
- met to PABA - allergies

Front 78

Lidocaine

Back 78

- HM to active metabolites
- many uses, intermediate duration

Front 79

Priolcaine

Back 79

- can cause methemoglobemia (lidocaine congener)

Front 80

Desipramine
Nortriptyline
Protriptyline

Back 80

- 2ary amine TCAs
- Block NE upakte > 5HT
- block Muscarinic (SLUDE), less H and Alpha block than 3ary

Front 81

Imipramine*
Amitriptyline
Trimipramine
Doxepin

Back 81

-3ary amines TCAs
- Block 5HT reuptake > 2ary amines
- also block muscarinic (SLUDE), H1, H2, & alpha 1 receptors
-decrease depression, suicidal tend, increase mood& appetite
*used to tx bedwetting (sphincter)

Front 82

Amoxapine

Back 82

-Heterocyclic antidepressant
- blocks NE> 5Ht
- fewer antichole S/Es
- S/E impotence, ARF, rarely used

Front 83

Maprotiline

Back 83

- secondary TCA, but has HIGH SEIZURE risk

Front 84

TCAS General

Back 84

- HMetabol, active metabolites
- Tx: depression, panic, phobias, OCD
- S/E: CV overstim, orthostatic hypo, reflex tachy, WEIGHT GAIN
-C/I: early recovery from MI, CVD, CHF
- tolerance to antichol effects devo; lots of DRUG reactions b/c additive side effects (sedation, hypotension, cardiotoxic, antichole)
- Do NOT use with MAOIs (CNS toxicity)

Front 85

Fluoxetine (prozac)
Paroxetine (paxil)
Sertaline (zoloft)
Fluvoxamine (Luvox)
Citalopram (celexa)
Escitalopram (lexapro)

Back 85

-SSRIs
- work at presynaptic terminal
- better S/E profile than TCAs
- wide therapeutic window
- HM by p450 system
- well absorbed, high protein binding

Front 86

Fluoxetine

Back 86

- most widely proscribed SSRI
- NO weight gain, or orthostatic hypotension, no antichole effects
- INHIBITS p450 isozymes
-S/e: GI, agitation, insomnia, minimal CV; may initially get worse!; sexual dysfunction

Front 87

SSRI + MAOI

Back 87

Serotonin Syndrome
- CNS toxicity due to flood of cleft, severe hypertension, hyperthermia, arrythmias, MS changes, seizures, can be deadly

Front 88

Tranylcypromine (R)
Phenelzine
Isocarboxazid

Back 88

- MAOIs, result in increase stores of monoamines
- not specific for MAO-A or B generally (B metabolizes DA)
- RE
- S/E: drowsy, hypotens, dry mouth; Tyramine also inactivated by MAO, so dietary restrict (hypertensive crisis)

Front 89

TX Hypertensive Crisis

Back 89

- decrease body temp
- short acting alpha 1 block or Ca block to drop blood pressure
- syx tx for N/v

Front 90

MAO poisoning

Back 90

-agigtation, hallucinations, hyperreflexia, seizures, hyperpyrexia

Front 91

MAO Drug Drug RXN

Back 91

Sympathomimetics & L-Dope: hypertensive crisis

TCAs: fever, delerium, serizures

Front 92

Buproprion

Back 92

- weak DA, NE, 5HT reuptake inhibitor
- few side effects, but can cause agitation, nausea, insomnia, seizures
- WEIGHT LOSS side effect used on purpose
- antidepressant and smoking cessation

Front 93

St. Johns Wort (Hypericum)

Back 93

-MAOI and 5HT reuptake inhibitor
-for mild or moderate depression

Front 94

Trazadone

Back 94

-SSRI used for insomnia b/c has substantial sedation effect
- no antichole side effects
- PRIAPISM

Front 95

Nefazodone

Back 95

- SNRI Blocks NE and 5HT reuptake
- good side effects (no sexual, no chole, no histamine0, but can be HEPATOTOXIC

Front 96

Venlafaxine
Duloxetine

Back 96

- SNRI (NE & 5HT reuptake blocker)
-better side effect profiles than TCAs

Front 97

Mirtazapine

Back 97

- TCA, stimulates NE/5Ht release by blocking autoreceptors (alpha2 and 5ht1)
- increased appetite and weight gain early on

Front 98

Lithium

Back 98

- mood stabilizer for bipolar
- MOA: reduces IP3, decreases CAMP, increases glutamate uptake, reduces response to 5HT & NE
- wide distribution, renal excretion (accumulates), LOW THERAPEUTIC INDEX (serum monitoring), watch Na levels also
-S/E: weight gain, tremors, inhibits ADH (polyuria/dips), hypothyroid effects

Front 99

Carbamazepine

Back 99

-anticonvulsant used for mood stabilization
- less side effects than lithium

Front 100

Valproate

Back 100

- anticonvulsant used for rapid cycling bipolar patients
-S/E: thrombocytopenia, monitor LFTs

Front 101

Lamotrigine

Back 101

- anticonvulsant used for mood stabilizing
- can cause Steven's Johnson

Front 102

Fluoxetine + Olanzapine

Back 102

- SSRI, antipsychotic combo for bipolar patients

Front 103

Omega 3s

Back 103

-decrease MAO-B
- found in walnuts, fish, canola
- def leads to less glucose delivery t oCNS

Front 104

Amphetamines

Back 104

- Amphetamine/Levo
- Dextroamphetamine
- Methamphetamine*
- Dextromethamphetamine
* more potent analog

Front 105

Amphetamines General

Back 105

- Tx: alleviate ADHD
- MOA: increase neurotran release (low Ne, mid Ne+DA, high NE, DA, 5HT), block reuptake, inhibit MAO
-Psychomotor stim, decrease appetite & weight
-S/e: over stim, convulsions
(chronic: schizo like state, damage neurons, tolerance), CV effects, can cause DIC, hyperthermia, GI probs
-TX OD with CHLORPROMAZINE to block DA/5HT receps, acidify urine

Front 106

Methylphenidate (ritalin0

Back 106

- related to amphetamines
- CNS stimulant, more effect on mental than motor, not as potent
- Tx: ADHA, paradoxically calming; nacrolepsy
-S/e: insomnia, anorexia

Front 107

Concerta

Back 107

- methylphenidate xtended release, not affected by food
- long duration of action

Front 108

Metadate CD

Back 108

- biphasic beads of methylphenidate for all day use

Front 109

Focalin

Back 109

- lower dose methylipheidate b/c different isomer

Front 110

Daytrana

Back 110

- Methylphenidate patch for kids

Front 111

Atomozetine (Strattera)

Back 111

- nonstimulant for ADAD
- NE reuptake inhibitor
-S/E: anorexia, N/V, insomnia, CAN'T USE WITH MAOIs

Front 112

Adderall

Back 112

-mixed amphetamine salt
-ADHD

Front 113

Dextroamphetamine

Lisdexamfetamine

Back 113

- single amphetamine salt

- prodrug of dextro

-ADHD

Front 114

Phentermine

Back 114

-Phen: increase release of DA
- Tx: obesity (with sibutramine)
- was used with fenfluramine (fenphen), but pulmonary hypertension, valve probs
-interacts with CYP3A4

Front 115

Sibutramine

Back 115

-inhibits reuptake of NE, 5HT, some DA
- Tx: obesity (with phentermine)
- AVOID with MAOI, SSSRI, LITHIUM, 5HT agonists

Front 116

MDMA (ecstasy)

Back 116

-MOA: indirect serotonergic agonist, increase release of 5HT, inhibits reuptake of 5HT
- sympatho&pyschomimetic
- S/e: narrow margin of safety, arrhythmias, hyperthermia, hepatic damage, depression with chronic use

Front 117

Cocaine

Back 117

- from cocoa plant
-MOA: inhibits reuptake of DA, NE, 5HT (esp DA), reduces capacity to transport all of them
-metabolized to BENZOYLECGONIE and ECGONINE also active; with ETOH to COCATHYLENE
- CNS stim, euphoria, sympathetic activation

Front 118

Cocaine Toxcitiy & Withdrawal

Back 118

Tox:
-IV propanolol if tachy is life threatening
-Nitroprusside or labetalol (hyperten)
-NaCL, catecholamines(hypoten)
-lidocaine (conduction)

W/d: bromocriptine (DA receptor agonist)

Front 119

Nicotine

Back 119

-plant alkaloid
- metabolized to COTININE rapidly
- MOA: activates cholinergic neurons in CNS/PNS: stim then block; inhibit MAO; activates release if NE/DA
OD: centeral resp paralysis, hypotension

Front 120

Caffeine

Back 120

-METHYLAXNTHINE, oral
- MAO: translocation of extrac Ca, increased CAMP, CGMP via block of adenosine receptors
-decrease fatigue, mild diuresis

Front 121

Theophylline

Back 121

-methylaxnthine found in tea, relaxes bronchiole smooth muscle

Front 122

Gamma Hydrobutyrate (GHB)
Flunitrazepam (BDZ)

Back 122

- date rape drugs; colorless, tasteless
- CNS depressant with SMALL THERAPEUTIC INDEX
-toxicity: amnesia, seizures, CV depr, coma, death

Front 123

Lysergic Acid Diethylamine (LSD)

Back 123

- 5HT1, 5HT2 agonist; activates sympathetic system
- hallucinationes, mood alterations
- block with HALOPERIDOL

Front 124

Phencycliden (PCP)

Back 124

-anatogonizes Glutamate action
- dissociative anethesia
- like ketamine

Front 125

Marijuana (delta THC)

Back 125

- receptors in basal ganglia, hippocampus, cerebellum
- euphoria, drowsiness, relax, memory impariment
- highly lipophilic
(Hashish is dried resin form, more potent)

Front 126

Dronabinol

Back 126

-Oral THC for Cancer chemo, AIDS pts

Front 127

Inhalents

Back 127

- cause axonopathies, hepatotoxic, cardiotoxic

Front 128

Mushrooms- Psilobycin

Back 128

-hallucinogenic
-dilated pupils, vertigo, psychotropic effects
- Tx: charcoal, diazepam

Front 129

L-Dopa

Back 129

-precursor of DA, txp into CNS, converted to DA by LaroAAdecarboxy
-lots of periperal LAAAD action, so need large doses, lots of SE (dyskinesia, hallucinations, N/V, arrhythmia), even stops working
-On-Off phemon with dosing
- DDRxn: B6 increases breakdown; MAOI hypertensive crisis

Front 130

Carbidopa

Back 130

-L-Dopa+ LAAAD inhibitor (Peripheral)
-increases availability, decreaes S/e, reduces dose of Ldopa
-Parkinsons

Front 131

Entacapone

Back 131

-COMT inhibitor
-adjunct to carbi/l-dop for on-off effects
-parkinsons

Front 132

Bromocriptine

Back 132

-adjunct with L-Dopa
-DA receptor agonist
- S/E are limiting: hallucinations, confusion, nausea
- less dyskinesia
-parkinsons

Front 133

Pramipexole (D3)
Ropinirole (D2)

Back 133

DA receptor agonists
- can delay need for L-dopa
- S/E: N/v, hallucination, insomnia, orthostatic hypo
-used to treat RLS, Parkinsons

Front 134

Amantidine

Back 134

-antiviral that enhances DA synthesis
- less effective than L-dopa, but less S/E; used as supplement
- better than anticholines on rigidity and bradykinesia
-parkinsons

Front 135

Selegiline

Back 135

- Selective MAO-B inhibitor (very selective so no hypertensive crisis risk)
- decreases oxidative stress
- reduces dose of L-dopa
needed
- metabolized to amphetamine, so DA potentiated in brain
-Parkinsons

Front 136

Trihexyphenidyl
Benzotropine
Biperiden

Back 136

-Antimuscarinic agents
- given prior to L-dopa to minimize side effects (adjunctive)
-parinsons

Front 137

Tolcapone

Back 137

- COMT inhibitor
- decrease on-off problem
-S/E of fulminant hepatic necrosis so limited use
-Parkinsons

Front 138

Huntingtons Disease

Back 138

- AD
- loss of GABA inhibition in striatum, hyperactive DA neurons in basal ganglia
- TX: DA anatgonists (Chlorpromazine, haloperidol); GABAb agonist (Baclofen)
*haloperidol also for tourettes

Front 139

Riluzole

Back 139

- for ALS, may protect neurons from glutamate
- prolongs time to trach
- ALS doesn't affect bladder or eye blink

Front 140

Tacrine

Back 140

- AchE-I for ALZ
-S/E: hepatotoxic, anorexia, diarrhea, nausea, fatigue
- LFTS have to be monitored
- with succinylcholine prolonged blockade

Front 141

Donepezil

Back 141

- AchE-I for ALZ, reversible non competitive
- less hepatotoxic
- mild to moderate ALZ
- with succinylcholine prolonged blockade

Front 142

Galantamine

Back 142

-AchE-i for ALZ, also has effects on nicotinic receptors
- NO hepatic effects
- with succinylcholine prolonged blockade

Front 143

Rivastigmine

Back 143

-AchE-i for Alz
- no hepatic effects
- inhibits butyrylcholinesterase also
- with succinylcholine prolonged blockade

Front 144

Memantine

Back 144

-NMDA antagonist
- treatment for severe ALZ

Front 145

Vit E

Back 145

Slows progression of ALz

Front 146

Interferon B-1a
Interferon B-1b

Back 146

-TX for MS, may interfere with INFg, slowing progression
- take early

Front 147

Glatiramer

Back 147

- for MS, inhibits immune response to myelin, may interfere with t-cell activation

Front 148

Mitoxantrone

Back 148

-antineoplastic used in MS to reduce relapses

Front 149

Baclofen
Methylprednisolone

Back 149

Antispasmodic, steroids given in acute exacerbations of MS

Front 150

Gout

Back 150

-purines metabolized to uric acid
- hyperuricemia (>6-7)
-idiopathic, renal retention, increased turnover, enzyme defects, low PH
- inflammatory repsonse to crystals
-avoid obesity, etoh, dehydration

Front 151

Cholchinie

Back 151

-inhibits phagocytosis, opsonization by leukocytes in Gout (MoA: binds to microtublues)
- decrease LA production, histamine, inflammatory glycos, inhibits LTAs
-S/e: GI

Front 152

Allopurinol

Back 152

- MoA: anti-Hypoxanthine, inhibits XO and blocks uric acid formation (low compet, high non-com)
- metabolite (alloxantine) non comp at all concent
- DOC in gout W/RF, STONES
- combo with chem (reduce 6MP b/c inhibits)
-combo with cholchinie when started b/c may cause acute attack

Front 153

Probenecid
Sulfinpyrazone

Back 153

- MoA: compet inhibit reabsorp of urate in PT, increase excretion
-S/e: GI (Sulf worse); can cause stones if not enough hydration, also add bicarb at start
- can use cholchine at start
- sulf inhibits PLT aggre (MI Tx?)

Front 154

Benzbromarone

Back 154

increases urate excretion (clinical trials)

Front 155

Phenylbutazone
Oxyphenylbutazone
Idomethacin
Sulindac
Naproxen

Back 155

-NSAIDs, reduce inflammation, pain

(NO asprin, decreases urate secretion)

Front 156

Tx for Status Epilepticus

Back 156

1)Iv benzo then Iv Phenytoin(fos)
2) Phenobarb
3) General Anesthesia (CP support)

Front 157

absence seizures

Back 157

-3Hz Spike wave pattern (saw tooth) in all lobes
-no aura, no postictal state (aura also absent in myoclonic)

Front 158

Antiepileptic mechanisms

Back 158

-inhibit Na or Ca influx (block depolar)
-augment GABA (add inhibit)
-inhibit Glutamate (block excite)

Front 159

Phenytoin (dilantin)

Back 159

- blocks Ca influx, Enhances Cl IPSPs to inhibit seizure spread, suppress epi focus
- DOC for all seizure XPT absence and atonic (will worsen)
-oral, high protein binding (IM causes necrosis), metabolism is RATE limited (enz is saturable)
-S/E: gingival hyperplasia, hirsuitism (ugly), stevens johnson, dose related CNS, fetal probs, give slow to avoid cardio probs (IV)
- INDUCES CYP3A4, give VitK

Front 160

Fosphenytoin

Back 160

-Prodrug of Pheytoin for seizures
- can give IM

Front 161

Carbamazepine (tegretol)

Back 161

-MoA unknown, but probably Decreases Na conductance
-tonic/clonic, partial, trigeminal neuralgia
- metabolite 10,11epoxide is active; POTENT INDUCER (incl own metabolism
- S/e: monitor LFTs, Na level (increases ADH), GI, Steven Johnson, blood counts!

Front 162

Phenobarbital

Back 162

-MoA: enhances GABA Cl flux so hyperpolarizes (makes refract longer)
-2nd line after pheny, prophy for febrile seizure
-INDUCES HEPATIC ENZS
-S/E: sedation (stupid); kids have hyperactivity, mental slowing; rashes

Front 163

Primidone

Back 163

-MoA: blocks Na channels; may also potentiate GABA b/c metabolized TO PHENOBARB & PEM
-combo with phenytoin often
-S/E: sedation; kids have hyperactivity, mental slowing; rashes; resp dep at high dose

Front 164

Valproic acid (depakote)

Back 164

-MoA: potentiates inhibitory GABA effects, blocks Na & K channels, inhibits T-Ca channels - BROAD spectrum
- Absence seizure (2nd line), reflex seizures, Bipolar disorder, etc
- INHIBITS P450s, so can cause toxicity of other drugs
-S/E: alopecia, weight gain, hepatic failure (LFTs)

Front 165

Ethosuximide

Back 165

-MoA:blocks T-Ca channels in thalamic interneurons
- ABSENCE seizures
-S/E: GI, CNS depression, Stevens Johnsons

Front 166

Lorazepam (IV)
Clonazepam (chronic)
Clorazepate (chronic)

Back 166

-Benzos: agonists at GABAa, block Na
- IV agents in status epilepticus
-S/E: sedation, anterograde amnesia; withdrawal seizures

Front 167

Ethotoin

Back 167

-adjunctive, fewer side effects
-shorter half life than phenytoin

Front 168

Mephytoin

Back 168

-for refractory pts
-risk of hepatotoxic, blood disorders

Front 169

Felbamate

Back 169

-enhances GABA, blocks glycine at NMDA
-ONLY for refractory partial seizures (Lennox-Gastaut synd)
-S/E: acute liver failure, aplastic anemia, GI, CNS, allergies in those predisposed (marketing killed it)

Front 170

Gabapentin (neurotin)

Back 170

-related to GABA, causes release of GABA from CNS, no effect of Rs
-adjunctive for partial seizures (weak), and to other drugs
-tx for neuralgia, DMneuropathy
-S/E: ataxia, dizzy, weight gain
- may be as good as carbamazepine monotherapy

Front 171

Pregabalin

Back 171

-binds Ca channels, modules NT release
- neuralgia, neuropathy, partial seziures

Front 172

Lamotrigine

Back 172

-inhibits voltage Na Channels (pheny, carba); inhibits glut release
-seizures, mood stabilizer
-S/e: cns, DIC, steven's johnson (high risk!), NOT used <16 yo
- induces own metabolism, affects other anti-seizure drugs

Front 173

Topiramate

Back 173

-inhibits volt Na channels; potentiates GABA at A; blocks AMPA excitatory; Carbonic anhydrase inhibitor
- seizures, LG syndrome, chronic headaches
-S/E: renal stones, weight loss (used for this off label), steven's johnson, GI, CNS - "Dopamax" b/c clouds mental

Front 174

Tiagabine

Back 174

-GABA reuptake inhibitor, inhibits GABA transporter
-partial seizures in adults and kids over 12
-S/E: CNS dep, GI, SJ rash

Front 175

Levetiracetam

Back 175

-unknown MoA, inhibits BURST firing
-adjunct in partial seizures, esp in patients with liver problems & on warfarin, cyclophos etc b/c no DDRs)
-S/E: CNS dep, pharyngitis, rhinitis, makes kids mean, expensive

Front 176

Oxcarbazepine

Back 176

-blocks Volt Na Channels to stabilize membranes
- medication resistant epil, partial seizures
- metab to active 10-hydroxycarbamezipine!
-NO autoinduction
-S/E: GI, CNS dep, SIADH

Front 177

Zonisamide

Back 177

-blocks Na channels, T-Ca channels
-partial seizures
-S/E: kidney stones, hepatic necrosis, anorexia, weight loss, SJrash, CNS slowing, aplastic anemia

Front 178

Vigabatrin

Back 178

-increases GABA by blocking GABA transaminase
- only available in Canada
-S/E weight gain, damage to cone photoreceptors

Front 179

Fetal Hydantoin Syndrome

Back 179

cleft lip, palate, congential heart disease, slowed growth, mental def

Front 180

Chlorpromazine (Thorazine)
(phenothiAZINES)

Back 180

-Schizophrenia drug (typical)
-MOA: competitive block of DA2>5Ht2 receps
-S/E:S/e bc block H1, M, A1 also (strong ACEffects - SLUDE); tardive, NMS, PRL, agranulo (CBCs), rabbit, weight, CI in SEIZURES
-lipophilic, abs erratic from GI; HM, RE
-improved motor effects; decrease positive syx
-used in intractable hiccups

Front 181

Thiothixene
(ThioXanTHENES)

Back 181

-typical antipsychotic (D2 more than 5HT)

Front 182

Haloperidol
(Butyrophenones)

Back 182

- competitive block of D2>D1>5Hts
- parental available
- more extrapyramidal S/E (mimic parkinsons); tardive, NMS; PRL; agranulo (CBCs), rabbit, weight
- DOC Tourettes, Huntington's

Front 183

Loxapine
(Azepine)
(Other azepines are atypical)

Back 183

-Typical antipsychotic (D2 more than 5HT)

Front 184

Molindone
(Dihydroindolone)

Back 184

-Typical Antipsychotic (D2 more than 5ht2)

Front 185

Trihexyphenidyl
Benztropine mesylate
Procyclidine HCl
Biperidin

Back 185

-anticholinergics
- Tx for EPS with antipsychotics

Front 186

Bromocriptine
Dantrolene

Back 186

-TX for NMS (also stop antipscychotic!)

Front 187

Prochlorperazine

Back 187

-antipsychotic used for DI nausea

Front 188

Scopolamine

Back 188

-antipsychotic is DOC for motion sickness

Front 189

Droperidol

Back 189

-antipsychotic is part of neurolepanesthesia

Front 190

Clozapine
Olanzapine
Quetiapine
(Azepines)

Back 190

- Atypical antipsychotics
- better for negative syx, refractory pts, less EPS, less tardive
- generally 5Ht2>>D2>D1>D4
- S/E: AGRANULOCYTOSIS (CBCs)

Front 191

Enkephalin
Endorphin
Dynorphin

Back 191

-proenkephalin (wide spread)
-POMC (localized, stress)
-pordynorphin (localized)

Front 192

MU receptor

Back 192

- potassium channel receptor (open, decrease cAMP)
- miosis, central (Supras) anesthesia, respir dep, euphoria, CV, GI, dependence
- Enkephalins, B-endorphin; Morphine, Fentanyl, Methadone, meperidine, buprenorphine

Front 193

Kappa Receptor

Back 193

- Ca receptor (block entry)
- miosis, spinal anesthesia, sedation, dysphoria
- Dynorphins; Butorphanol, Pentazocine, Nalbuphine

Front 194

Delta Receptor

Back 194

- Potassium channel receptor (open, decrease cAMP)
- affective behavior
- enkephalins, B-endorphin; no drugs

Front 195

Morphine

Back 195

- from opium (morphine, codeine, papverine), synthetics (heroin, nalorphine, naloxone, naltrexone)
- potent AGONIST at Mu>>>delta
- MIOSIS, CONSTIPATION, direct respire dep, analgesia, euphoria, antitussive (medulla)
- C/I gallstones

Front 196

Codeine/Hydrocodone

Back 196

-cough suppressant at doses lower than as analgesic (decrease sens to stimuli)
- NALOXONE antagonizes)

Front 197

Oxycodone/Ibuprofen
Oxycodone/Aspirin
Oxycodone/acetaminophen

Back 197

-Combunox
-Percodan
-Percocet

Front 198

Dextromethorphan

Back 198

-synthetic derivative of morphine, suppresses cough center
- no analgesic or addictive
- NOT mu receptor mediated, so Naloxone doesn't block

Front 199

Diphenoxylate
Loperamide

Back 199

-antidiarrheal via mu receps in GI SM

Front 200

Opiate metabolism

Back 200

- HM, RE
- lots of active mets
- heroin to 6-monoacetylmorphine* (drug screen)
- 6-mono to morphine
- codeine to morphine
- morphine to Mor-6-gluc
- C/I: hepatic probs, Respir probs

Front 201

Opiates

Back 201

- potentiated by phenothiazines, MOAis, TCAs
- withdrawal get rebound (dialation, diarrhea, dysphoria, hypervent)
- poisoning: pinpoint pupils, coma, resp depression (TX iv naloxone)

Front 202

Naloxone
Nalmefene (more potent)
Naltrexone (oral, for Etoh)

Back 202

- mu receptor ANTAGONISTS, used to tx opiod OD, prevent dependence
- can induce W/D in dep subjects

Front 203

Meperidine

Back 203

- synthetic phenylpiperidine
- less potent Mu AGONIST
- CNS probs (seizs) at toxic b/c of NORMEPERIDINE metabolite
- NOT blocked by naloxone
- no antitussive, better bioavail than morphine, tolerance slower
- C/I MAOIs (Demerol)

Front 204

Fentanyl

Back 204

- Mu receptor AGONIST
- synthetic phenylpiperdine analgesic
- merperidine analog
- 80X as potent as morphine
- patch or IV
- less nausea
-C/I: MAOIs

Front 205

Sufentanil

Back 205

- fentanyl derivative
- 6000 X as potent as morphine
- IV, anesthesia adjunct (less hemodynamic instability, less respir depression)
- costly

Front 206

Alfentanil

Back 206

- fentanyl derivative
- 40X as potent as morphine
- post op anesthesia

Front 207

Alfentanil

Back 207

- Mu AGONIST
- short acting, more potent than alfentanil

Front 208

Methadone

Back 208

- Mu AGONIST
- effect analgesic
-S/E: biliary spasms, constipation
-used in W/D for heroin, opiates

Front 209

Propoxyphene

Back 209

- weak Mu AGONIST
- analgesic, combo with aceta or aspirin
-less potential for abuse or dependence
(Darvon)

Front 210

Pentazocine

Back 210

- mixed Mu ANTAGONIST, Kappa AGONIST
- analgesia, sedation, resp depression
- used for acute pain treatment
- naloxone added to prevent abuse (can block morphine, precip w/d alone)
- psychotomimetic effects
-benzomorphone

Front 211

Buprenorphine

Back 211

-Mu partial AGONIST, Kappa ANTAGONIST
-less effective analgesic, but very long half life
-used to treat opiod dependecne

Front 212

Tramadol

Back 212

- binds opiod receptors but chemically unrelated
- inhibits 5HT, NE reuptake
-constipation, nausea, dizzy, drowsy
- partially blocked by naloxone
- oral for moderate pain

Front 213

Gell & Coombs

Back 213

I: IgE, <30 mins, anaphylactic
II: IgM/IgG, 5-12 hours, antigen
III: Complement, 3-8 hours, immune complexes
IV: T-cells, 24-28 hrs, cell mediated

Front 214

Serum Sickness

Back 214

- soluable circulating immune complexes (III)
- fever, malaise, lymphadenop
- 7-14 days
- Cefaclor, antivenoms, cephalosporins

Front 215

Drug Fever

Back 215

- antibiotics, amphi B

Front 216

Drug Induced SLE

Back 216

-Hydrazine
-Isoniazid
-Procainamide
-Phenytoin

Front 217

Renal Interstitial Neph

Back 217

-fever, rash, EOS
-humoral AB based RXN, may be to basement
-Methicillin (antistaphs), cimetidine, Sulfonamides

Front 218

Toxic Hepatitis

Back 218

- fever, rash, granulomas, EOS
- Erythromycin, PCNs, Allopurinol, Sulfonamides

Front 219

Vasculitis

Back 219

- palpable purpuric lesions
- anticoagulants, allopurinol, PCNs

Front 220

Maculopapular Rash

Back 220

- anticonvulsants, PCN, NSAIDs,

Front 221

Angioedema

Back 221

- ACE inhibitors, phenytoin

Front 222

Fixed-drug eruption

Back 222

- lesions in same place all the time
- NSAIDs, ABX

Front 223

Phototoxicity/Allergy

Back 223

- sunburn (energy)/rash (hapten)
- Tetracyclines, OCPs, Phenothiazines

Front 224

Erythema Multiform

Back 224

-target lesions
-hands, feet then elsewhere, URI syx
- anticonvulsants, NSAIDs, PCNs

Front 225

Stevens-Johnson

Back 225

- severe EM, skin lesions with large bullae, keratitis, need to go to burn unit
- Sulfonamides, Anticonvulsants, NSAIDs

Front 226

TEN

Back 226

- malasise fever, EM to SJ to TEN fast
- large bullae, ski sloughs off in large sheets, have to go to burn unit (sepsis, lytes, fluids, infx)
- Anticonvulsants, Sulfonamides

Front 227

Pulmonary

Back 227

Rhinitis/Asthma
-NSAIDs, sulfites, Betablock
Acute infiltrate
- Nitrofurantoin, bleomycin, gold

Front 228

Hematological

Back 228

Eos: Digitalis, ABx
Aplastic Anemia: pancytopenia, fatigue, bruising
- dose dep (chemo)
- idiopathic (choramphenicol!)
- anticonvulsants, chloram.

Front 229

Hemolytic Anemia

Back 229

- Drug binding to RBCs, so abs destroy it: PCNs, cephs
- immune complexes in serum: phenacetin, quinidine
- IgG antidrug metabolite binds RBC directly: methyldopa, levodopa, procainamide, nitrofurantoin (COOMBS +)

Front 230

Thrombocytopenia

Back 230

-bind to PLT (heparin)
-complexes in serum (quinidine)
-drug+HLA antigens on PLTS (Gold Salts)

Front 231

Angranulocytosis

Back 231

-chills, fever, sore throat, collapse
-binding to PMN: PCNs
-complexes in serum: quinidine
-hapten
-alterations in PMN membrane
- Cloropromazine, methyldopa, procainmide, caramezepine

Front 232

Derm Pharm Points

Back 232

- Percutaneous absorption= diffusion
- Permeation through stratum corneum is rate limiting
- infants have surface/body weight ratio 3x adult

Front 233

Fick's Diffusion law

M = DCT/ H

Back 233

M= drug in receptor phase
D= Diffusion
C= concentration
T= time
H= thickness (inverse!)

Front 234

Diffusion Eq #2

J = KmDm/Th C

Back 234

J= amount penetrating
Km= solubility
Dm= diffusion coeff
C= concentration grad
Th= thickness (inverse!)