Reverse pharm-CNS Flashcards by Tim Horrocks

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

How well did you know this?

Not at all

Perfectly

alpha 2 agonist

Decr. aq. humor synth

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

brimonidine

How well did you know this?

Not at all

Perfectly

Beta blockers

decr. aque humor synth

No pupillary or vision changes

timolol, betaxolol, carteolol

How well did you know this?

Not at all

Perfectly

Diuretic

Decr. aq humor synth via inhibition of carb. anhydrase

No pupillary or vision changes

acetazolamide

How well did you know this?

Not at all

Perfectly

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

How well did you know this?

Not at all

Perfectly

InDirect cholinomimetics (2)

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

Miosis and cyclospasm

Physostigmine and echothiophate

How well did you know this?

Not at all

Perfectly

Prostaglandin (PGF2alpha)

Incr. outflow of aq humr

Darkens color of iris (browning)

latanoprost

How well did you know this?

Not at all

Perfectly

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?

How well did you know this?

Not at all

Perfectly

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

How well did you know this?

Not at all

Perfectly

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

Chronic pain

Similar to opioids. Decreases seizure threshhold. Serotonin syndrome.

tramadol

How well did you know this?

Not at all

Perfectly

Blocks thalamic T type Ca channels

Absence (first line)

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

Ethosuximide

How well did you know this?

Not at all

Perfectly

Status epilepticus (acute 1st line)
Eclampsia

Incr. GABA-A action

Sedation, tolerance, dependence, resp. depression

Benzos

How well did you know this?

Not at all

Perfectly

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

How well did you know this?

Not at all

Perfectly

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

How well did you know this?

Not at all

Perfectly

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

How well did you know this?

Not at all

Perfectly

Simple, complex
periph neuro
postherpetic neuralgia

Primarily inhibits high voltage gated Ca channels: GABA analog

Sedation, ataxia

Gabapentin

How well did you know this?

Not at all

Perfectly

Simple, complex, tonic clonic
1st line in neonates

Incr. GABA-A action

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

Phenobarbital

How well did you know this?

Not at all

Perfectly

simple, complex, tonic clonic
Migraine prevention

Blocks Na channels
Incr. GABA action

Sedation, mental dulling, kidney stones, weight loss

topiramate

How well did you know this?

Not at all

Perfectly

Simple, complex, tonic clonic, absence

Blocks voltage gated Na channels

SJS

Lamotrigine

How well did you know this?

Not at all

Perfectly

simple, complex, tonic clonic

unknown; may modulate GABA and glutamate release

Levetiracetam

How well did you know this?

Not at all

Perfectly

simple, complex

Iincr. GABA by inhibit uptake

Tiagabine

How well did you know this?

Not at all

Perfectly

simple, complex

Incr. GABA by irreversibly inhib GABA transaminase

Vigabatrin

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

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

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)

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

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

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

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

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)

IV anesthetics

barbituates, benzos, ketamine, opioids, and propofol?

barbituate High potency/lipid solubility High blood solubility/rapid induction and recovery Induction of anesthesia and short surgical procedures Decr. cerebral blood flow

Thiopental

Benzo Endoscopy Gaseous anesthetics and narcotics Severe post op resp depression Decr. BP Anterograde amnesia

Midazolam

Arylcyclohexylamines=PCP like Block NMDA receptors Dissociative anesthetics CV stim disorientation hallucination bad dreams incr. CBF

Ketamine

Opioids (2) Used with other CNS depressants during general anesthesia

Fentanyl, morphine

Potentiates GABA-A Sedation in ICU Rapid anesthesia induction short procedures Less post op nausea

Propafol

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)

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

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

Prevents release of Ca from the SR of skel muscle Malignant hyperthermia and NMS

Dantrolene

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

Baclofen

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

Cyclobenzaprine

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

Dopamine agonists

Incr. DA release and decr. reuptake Ataxia livedo reticularis

Amantadine

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

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

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

Antimuscarinic Improves tremor and rigidity, not bradykinesia

Benztropine

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

NMDA receptor antag; helps prevent excitotoxicity Alzheimers Dizziness confusion hallucinations

Memantine

AChE inhibitors Alzheimers Nausea, dizziness, insomnia

donepezil, galantamine, rivastigmine

Inhibit vesicular monoamine transporter (VMAT) Limit DA vesicle packaging and release (1/2) D2 receptor antagonist )3 Huntingtons

Tetrabenzine and reserpine | Haloperidol

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