Reverse pharm-CNS Flashcards Preview

Step One > Reverse pharm-CNS > Flashcards

Flashcards in Reverse pharm-CNS Deck (53):
1

alpha 1 agonist

Decr. aqueous humor secretion by vasoconstriction

Mydriasis; don't use in closed angle glaucoma

Blurry vision, ocular hyperemia, foreign body sensation, ocular allergic reactions, cular pruritus

epinephrine

2

alpha 2 agonist

Decr. aq. humor synth

lurry vision, ocular hyperemia, foreign body sensation, ocular allergic reactions, cular pruritus

brimonidine

3

Beta blockers

decr. aque humor synth

No pupillary or vision changes

timolol, betaxolol, carteolol

4

Diuretic

Decr. aq humor synth via inhibition of carb. anhydrase

No pupillary or vision changes

acetazolamide

5

Direct cholinomimetics (2)

Incr. outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular mesh

Miosis and cyclospasm

Use 1 in emergencies-very effective at opening meshwork into canal of schlemm

Pilocarpine (1) and carbachol

6

InDirect cholinomimetics (2)

Incr. outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular mesh

Miosis and cyclospasm

Physostigmine and echothiophate

7

Prostaglandin (PGF2alpha)

Incr. outflow of aq humr

Darkens color of iris (browning)

latanoprost

8

Opioid analgesics (11)

Agonists at opioid receptors (mu=morphine, delta=enkephalin, kappa=dynorphin) to modulate synaptic transmission (open k+ channels, close Ca channels) leading to decr. synaptic transmission. Inhibit release of ACh, NE, 5-HT, glutamate, and substance P

1=cough suppresion (1)
2=diarrhea (2)
3=maintenance programs for heroin addicts (3)

pain, acute PE

Addiction, resp. depression, constipation, miosis, additive CNS depression w/ other drugs.

Tolerance does not develop to constipation and miosis

Naloxone or naltrexone (opiod receptor antag)

What kind of drugs are dextromethorpan (1), loperamide/diphenoxylate (2), methadone/buprenorphine + naloxone (3), morphine, fentanyl, codein, meperidine, pentazocine? What is their mechanism? What is their clinical use overall? Of 1? 2? 3? What is their toxicity? How is toxicity treated? Mech? Which sx does tolerance develop to?

9

Kappa opioid receptor agonist and mu opioid receptor partial agonist; produces analgesia

Severe pain (migraine/labor).

Causes less resp. depression than full agonist

Can cause opioid withdrawal symptoms if pt. is also taking full agonist
Overdose not easily reversed w/ naloxone

butorphanol

10

Very weak opioid agonist; also inhibits 5-HT and NE reuptake

Chronic pain

Similar to opioids. Decreases seizure threshhold. Serotonin syndrome.

tramadol

11

Blocks thalamic T type Ca channels

Absence (first line)


Fatigue
GI Distress
Headache
Itching (urticaria)
Stevens-Johnson syndrome

Ethosuximide

12

Status epilepticus (acute 1st line)
Eclampsia

Incr. GABA-A action

Sedation, tolerance, dependence, resp. depression

Benzos

13

Simple, complex, tonic clonic (first line), status epilepticus (prophylaxis first line)

Incr. Na channel inactivation; zero order kinetics

Nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, periph neuro, megaloblastic anemia, teratogenesis, SLE like syndrome, induction of cytochrome p450, SIADH, SJS

Phenytoin

14

Simple, complex, tonic clonic (all first line)
1st line for trigeminal neuralgia

Incr. Na channel inactivation

Diplopia, ataxia, blood dyscrasias, liver toxicity, teratogenesis, induction of p450, SIADH, SJS

Carbamazepine

15

Simple, complex, tonic clonic (first line), absence, myoclonic seizures, BPD

Incr. na channel inactivation
Incr. GABA conc. by inhibiting GABA transaminase

GI, distress, rare but fatal hepatotoxicity, neural tube defects, tremor, weight gain, CI in pregnancy

valproic acid

16

Simple, complex
periph neuro
postherpetic neuralgia

Primarily inhibits high voltage gated Ca channels: GABA analog

Sedation, ataxia

Gabapentin

17

Simple, complex, tonic clonic
1st line in neonates

Incr. GABA-A action

Sedation, tolerance, dependence, induction of P450, cardioresp depress

Phenobarbital

18

simple, complex, tonic clonic
Migraine prevention

Blocks Na channels
Incr. GABA action

Sedation, mental dulling, kidney stones, weight loss

topiramate

19

Simple, complex, tonic clonic, absence

Blocks voltage gated Na channels

SJS

Lamotrigine

20

simple, complex, tonic clonic

unknown; may modulate GABA and glutamate release

Levetiracetam

21

simple, complex

Iincr. GABA by inhibit uptake

Tiagabine

22

simple, complex

Incr. GABA by irreversibly inhib GABA transaminase

Vigabatrin

23

Prodrome of malaise and fever followed by rapid onset of erythematous/purpuric macules (oral, ocular, genital)

Skin lesions progress to epidermal necrosis and sloughing

SJS

24

First line drugs for what?

carbamazepine
carbamazepine
phenytoin, carbamazepine, valproic acid
ethosuximide
benzos
phenytoin

Simple=carbamazepine
complex=carbamazepine
tonic clonic=phenytoin, carbamazepine, valproic acid
absence=ethosuximide
Status Epilepticus acute=benzos
SE proph=phenytoin

25

Barbituates (4)

Facilitate GABA-A action by incr. duration of Cl- channel opening, decr. neuron firing

Sedative for anxiety, seizures, insomnia, induction of anesthesia (1)

Resp. and CV depression
CNS depression (worse with alcohol)
Dependence
Induces P450
Overdose treatment is support

Not in porphyria

Phenobarbital, pentobarbital, secobarbital, thiopental (1)

26

Long acting benzos=less abuse potential

Facilitate GABA-A action by incr. freq. of Cl- opening.
Decr. REM sleep

Anxiety, spasticity, Status epilepticus (1/2), detoxification (DTs), night terrors, sleepwalking, general anesthetic (amnesia, muscle relax), hypnotic (insomnia)

Dependence, additive CNS depression effects with alcohol, less risk of resp depression than with barbituates.

Flumazenil for overdose (comp antag)

1=diazepam
2=lorazepam
temazepam
Chlordiazepoxide

27

short acting benzos=less abuse potential

Facilitate GABA-A action by incr. freq. of Cl- opening.
Decr. REM sleep

Anxiety, spasticity, detoxification (DTs), night terrors, sleepwalking, general anesthetic (amnesia, muscle relax), hypnotic (insomnia)

Dependence, additive CNS depression effects with alcohol, less risk of resp depression than with barbituates.

Flumazenil for overdose (comp antag)

Alprazolam
Triazolam
Oxazepam
Midazolem

28

All ZZZs put you to sleep

Act via the BZ1 subtype of GABA receptor (flumenazil reverses it)

Insomnia

Ataxia, headaches, confusion.
Only modest day after psychomotor depression
Decr. dependence risk than benzos
Rapid metabolism (short acting)

Zolpidem, Zaleplon, eszopiclone

29

1 has decr. blood and lipid solubility=low potency and fast induction

2 has incr. lipid and blood solubility=High potency and slow induction

1=N2O
2=Halothane

30

Inhaled anesthetics

Mechanism unknown

Myocardial depression
respiratory depression
nausea/emesis
Incr. cerebral blood flow (decr. cerebral metabolic demand)

1-hepatotoxicity
2-proconvulsant
3-nephrotoxicity

All but 3=malignant hyperthermia: life threatening hereditary condition in which inhaled anesthetics with succinylcholine induce fever and severe muscle contractions

halothane (1), enflurane (2), isoflurane, sevoflurane, methoxyflurane, and N2O (3)

31

IV anesthetics

barbituates, benzos, ketamine, opioids, and propofol?

32

barbituate

High potency/lipid solubility
High blood solubility/rapid induction and recovery

Induction of anesthesia and short surgical procedures

Decr. cerebral blood flow

Thiopental

33

Benzo

Endoscopy
Gaseous anesthetics and narcotics

Severe post op resp depression
Decr. BP
Anterograde amnesia

Midazolam

34

Arylcyclohexylamines=PCP like

Block NMDA receptors

Dissociative anesthetics

CV stim
disorientation
hallucination
bad dreams

incr. CBF

Ketamine

35

Opioids (2)

Used with other CNS depressants during general anesthesia

Fentanyl, morphine

36

Potentiates GABA-A

Sedation in ICU
Rapid anesthesia induction
short procedures

Less post op nausea

Propafol

37

1-3=Ester local anesthetic
4-6=amide anesthetic (2 I's)

Blocks Na channels by binding specific receptors on iner portion of channel.
Preferentially binds to activated Na channels, so most effective in rapidly firing neurons
Tertiary amine local anesthetics penetrate membrane in uncharged form, then bind to ion channels as charged form.

Given with vasoconstrictors (epi) to enhance local action (it won't dilute away)
In infected tissue (acidic), must use more
small myel >small unmyel > large myeli =n > large unmyel

Pain > temp > touch > pressure

Minor surgical procedures
Spinal anesthesia
If allergic to esters, give amide

CNS excitation, severe CV toxicity (6), hypertension, hypotension, arrythmias (2), methemoglobinemia (benzocaine)

procaine, cocaine, and tetracaine (1-3)? Lidocaine, mepivicaine, bupivacaine (4-6)

38

Depolarizing NM blocking drug; strong ACh receptor agonist

Produces sustained depolarization and prevents muscle contraction.

Muscle paralysis in surgery or mech ventilation
Selective for motor (vs. autonomic) nicotinic receptor

Hypercalcemia, hyperkalemia, malignant hyperthermia

Succinylcholine

39

Non depolarizing NM blocking drug

Competitive antag at ACh receptor

Muscle paralysis in surgery or mech ventilation
Selective for motor (vs. autonomic) nicotinic receptor

Reversal-Neostigmine (with atropine to prevent musc effects), edrophonium, and other cholinesterase inhib.

tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium

40

Prevents release of Ca from the SR of skel muscle

Malignant hyperthermia and NMS

Dantrolene

41

Inhibits GABA-B receptors at spinal cord level, inducing skel muscle relaxation

Muscle spasms

Baclofen

42

Centrally acting skel muscle relaxant. Structurally related to TCAs, similar anticholinergic side effects.

Muscle spasms.

Cyclobenzaprine

43

Ergot-bromocriptine
Non ergot (preferred)-pramipexole, ropinirole

Dopamine agonists

44

Incr. DA release and decr. reuptake

Ataxia
livedo reticularis

Amantadine

45

Blocks periph conversion of L-DOPA to dopamine by inhibiting DOPA decarboxylase

More L-DOPA in CNS
Reduces side effects of periph dopamine (N/V)

Carbidopa

46

Selectively inhibits MAO-B, which preferentially metabolizes DA over NE and 5-HT.
DA isn't converted to 3-MT and thus more is available in brain

Adjunctive agent to L-dopa i treatment of park disease

Selegeline

47

Prevent peripheral Ldopa degradation to 3-O-methyldopa by inhibiting COMT

1-blocks conversion of dopamine to DOPAC by inhibiting CENTRAL COMT

1=tolcapone
entacapone

48

Antimuscarinic

Improves tremor and rigidity, not bradykinesia

Benztropine

49

Incr. level of DA in brain. It can cross BBB and is converted by Dopa decarboxylase in the CNS to DA. Used with carbidopa.

parkinsons

Arrhythmias from periph formation of catecholamines
Long term use can lead to dyskinesia following administration, akinesia b/w doses.

L Dopa

50

NMDA receptor antag; helps prevent excitotoxicity

Alzheimers

Dizziness
confusion
hallucinations

Memantine

51

AChE inhibitors

Alzheimers

Nausea, dizziness, insomnia

donepezil, galantamine, rivastigmine

52

Inhibit vesicular monoamine transporter (VMAT)
Limit DA vesicle packaging and release (1/2)

D2 receptor antagonist )3

Huntingtons

Tetrabenzine and reserpine
Haloperidol

53

5-HT-1B/1D agonist
Inhibit CNV activation
Prevent vasoactive peptide release
Induce vasoconstriction

Acute migraine
Cluster headaches

coronary vasospasm (CI in CAD or prinzmetal angina)
Mild paresthesia

Sumatriptan