Mech: vasoconstr (α1) → decr. aq. humor synth (vasoconstriction)

Tox: mydriasis (α1), stings

Contra: closed-angle glauc (do NOT use)

α-Ag

Mech: vasoconstr → decr. aq. humor synth

Use: glauc

Note: no pupil/vision chg.

β-blocker (others: betaxolol, carteolol)

Mech: decr. aq. humor secr

(Blocks β-activation of Ciliary process)

Tox: Systemic β-blocker (bradycardia)

Note: no pupil/vision chg.

CA inhibitor diuretic

Mech: decr. HCO3- → decr. aq humor secr

Note: no pupil/vision chg.

(direct) Cholinomimetic

Mech: contract ciliary m. (lens relaxes) & open trabecular mesh/canal of Schlemm → incr. aq humor outflow

Use: glauc emergencies

Tox: Miosis (M3), cyclospasm

(direct) Cholinomimetic

Mech: contract ciliary m. (lens relaxes) & open trabecular mesh/canal of Schlemm → incr. aq humor outflow

Use: glauc

Tox: Miosis (M3), cyclospasm

(indirect) Cholinomimetic

Mech: contract ciliary m. (lens relaxes) & open trabecular mesh/canal of Schlemm → incr. aq humor outflow

Use: glauc

Tox: Miosis (M3), cyclospasm

(indirect) Cholinomimetic

Mech: contract ciliary m. (lens relaxes) & open trabecular mesh/canal of Schlemm → incr. aq humor outflow

Use: glauc

Tox: Miosis (M3), cyclospasm

PGF2α

Mech: incr. outflow of aq humor thru uveoscleral tract (not canal of Schlemm)

Tox: darkens iris (browning)

Opioid - μ Ag

Mech: opens K chan (postsyn), closes Ca chan (presyn) →decr. synaptic transm (dec. ACh NE 5HT subP gluta)

Use: pain, acute pulm edema

Tox: resp/CNS depression, constip, pinpoint pupils; sphincter of Oddi sm. m. constrict → biliary colic

Antidote: naloxone or naltrexone (μ-antag)

Note: tolerance does not devel to miosis & constip 

Opioid - μ Ag

Mech: opens K chan (postsyn), closes Ca chan (presyn) →decr. synaptic transm (dec. ACh NE 5HT subP gluta)

Use: pain, acute pulm edema

Tox: resp/CNS depression, constip, pinpoint pupils; sphincter of Oddi sm. m. constrict → biliary colic

Antidote: naloxone or naltrexone (μ-antag)

Note: tolerance does not devel to miosis & constip

Opioid - μ Ag

Mech: opens K chan (postsyn), closes Ca chan (presyn) →decr. synaptic transm (dec. ACh NE 5HT subP gluta)

Use: pain, acute pulm edema

Tox: resp/CNS depression, constip, pinpoint pupils; sphincter of Oddi sm. m. constrict → biliary colic

Antidote: naloxone or naltrexone (μ-antag)

Note: tolerance does not devel to miosis & constip

Varied CYP2D6 - over/under metabolizers
of codeine to morphine. (2D6 blocked by fluoxitine and diphenhydramine)

Opioid - μ Ag

Mech: opens K chan (postsyn), closes Ca chan (presyn) →decr. synaptic transm (dec. ACh NE 5HT subP gluta)

Use: pain, acute pulm edema

Tox: resp/CNS depression, constip, pinpoint pupils; sphincter of Oddi sm. m. constrict → biliary colic

Antidote: naloxone or naltrexone (μ-antag)

Note: tolerance does not devel to miosis & constip

Fastest Onset Opioid - most euphoria

Opioid - μ Ag

Mech: opens K chan (postsyn), closes Ca chan (presyn) →decr. synaptic transm (dec. ACh NE 5HT subP gluta)

Use: Maintinence for Addicts pain, acute pulm edema

Tox: resp/CNS depression, constip, pinpoint pupils; sphincter of Oddi sm. m. constrict → biliary colic

Antidote: naloxone or naltrexone (μ-antag)

Note: tolerance does not devel to miosis & constip

Slow Onset Opioid (no euphoria)

Opioid - μ Ag (Demerol)

Mech: opens K chan (postsyn), closes Ca chan (presyn) →decr. synaptic transm (dec. ACh NE 5HT subP gluta)

Use: pain, acute pulm edema

Tox: resp/CNS depression, constip, pinpoint pupils; sphincter of Oddi sm. m. constrict → biliary colic

Antidote: naloxone or naltrexone (μ-antag)

Note: tolerance does not devel to miosis & constip

Low Potency, inc risk seizure, delirium not used much

Opioid - μ Ag/NMDA antag

Mech: opens K chans (postsyn), closes Ca chans (presyn) → decr. synaptic transm

Use: pn, acute pulm edema; cough suppression

Tox: resp depression, constip, pinpoint pupils, CNS depression; sphincter of Oddi sm. m. constrict → biliary colicAntidote: naloxone or naltrexone (μ-antag)Note: tolerance does not devel to miosis & constip 

Opioid - μ Ag

Mech: opens K chan (postsyn), closes Ca chan (presyn) →decr. synaptic transm (dec. ACh NE 5HT subP gluta)

Use: Diarrhea

Tox: resp/CNS depression, constip, pinpoint pupils; sphincter of Oddi sm. m. constrict → biliary colic

Antidote: naloxone or naltrexone (μ-antag)

Note: tolerance does not devel to miosis & constip

Opioid - μ Ag

Mech: opens K chan (postsyn), closes Ca chan (presyn) →decr. synaptic transm (dec. ACh NE 5HT subP gluta)

Use: Diarrhea

Tox: resp/CNS depression, constip, pinpoint pupils; sphincter of Oddi sm. m. constrict → biliary colic

Antidote: naloxone or naltrexone (μ-antag)

Note: tolerance does not devel to miosis & constip

μ-partial Ag  κ-Ag

Use: pnTox: causes w/d if on full opioid ag;

less resp depr than full ag

κ = dynorphin opioid receptor (disassociative & disphoria)

Weak opioid ag/ 5-HT & NE reuptake inhib

Use: chronic pn

Tox: opioid tox; decreases seizure threshold

Epilepsy drug

Mech: Na chan inactivation

Use: 1st line for T-C; 1st line for trigeminal neuralgia

Tox: diplopia, ataxia, blood dyscrasias, hepatotox, teratogen. Stephen-Johnson SIADH

Interact: (+) P-450

Epilepsy drug

Mech: blocks thalamic T-type Ca chans

Use: 1st line for absence seizures

Tox: GI, Stevens-Johnson synd

Epilepsy drug

Mech: Na chan inactivation; incr GABA conc

Use: 1st line for T-C; myoclonic seizures

Tox: GI, fatal hepatotox (monitor LFTs), neural tube defects (contra: preg), tremor

Epilepsy drug

Mech: blocks voltage-gated Na chans (cant depolarze)

Tox: Stevens-Johnson synd

Epilepsy drug

Mech: GABA analogue; inhibits HVA (high voltage activated) Ca channels.

Use: seizures; periph neuropathy, bipolar

Tox: sedation, ataxia

Epilepsy drug

Mech: Blocks Na chans; incr. GABA action

Tox: sedation, kidney stones, wt. loss

Epilepsy drug

Mech: Na chan block; inhibs Glu release

Use: 1st line for T-C seizures; 1st line for status epilepticus prophyl; class IB (Na) antiarrhythmic

Tox: nystagmus, diplopia, SLE-like synd, gingival hyperplasia (kids), peripheral neuropathy, hirsutism, megaloblastic anemia (decr. folate abs), teratogen (fetal hydantoin synd)

Interact: (+) P-450 

Barbiturate (others: pentobarbital, thiopental, secobarbital)

Mech: incr. duration of Cl chan opening → facilitate GABAA (receptor) action

Use: anx, seizures, insomnia; 1st line in preg/kids; induction agent (thiopental)

Tox: additive CNS depression w/ alc; resp depression

Interact: (+) P-450

Note: no antidote - tx OD w/ sx management (assist resp, incr. BP)

Benzo (lorazepam, triazolam, temazepam, midazolam)

Mech: incr. freq of Cl chan opening → facilitate GABAA; decr. REM & delta sleep

Use: anx, acute status epilepticus, detox (delirium tremens), night terrors, sleep walking

Tox: additive CNS depression; less risk of resp depression/coma than barbs

Antidote: flumazenil (comp antag)

Short Acting: Oxazepam, Triazolam, Midazolam.

Inhaled anesthetic (others: enflurane, isoflurane, NO)

Effects: CV/resp depression, n/v, incr. cerebral blood flow (decr. metab demand)

Tox: hepatotox (halothane), nephrotox (methoxyflurane), convulsions (enflurane), malign hyperthermia (give dantrolene)

Barbiturate - IV anesthetic (high potency, high sol)

Use: induction & short surg

Note: decr. cerebral blood flow (unlike inhaled anesth)

BZ - IV anesthetic

Use: endoscopy; adjunct w/ gas anesth/narcs

Tox: postop resp depression, decr. BP, amnesia

PCP analog/dissociative anesthetic

Mech: NMDA blocker (halucinagen); cardio stim

Tox: disorientation, hallucination, bad dreams

Note: incr. cerebral blood flow (sim. to inhaled anesth)

= Special K

Opiate - IV anesth (others: morphine)

Use: combine w/ other CNS depressants during general anesth

Mech: potentiates GABAA

Use: rapid induction & short surg

Tox: less postop nausea than thiopental (no hangover)

Local Ester anesthetic  (cocaine, tetracaine bupivacaine)

Mech: 3o amines penetrate membr → become charged (locked in) → block Na chans from the inside (preferentially bind activated chan)

Use: minor surg, spinal anesth;

if allergic to esters, give amides.

Tox: HTN/hypoTN, arrhythmias (coke)

Notes: 1) cannot penetrate membr in infected (acidic) tissue → req incr. dose;

2) order lost: pn- Temp- touch- Press; small /mylelinated before large/ unmyleinated(# Ca chan)

3) given w/ vasoconstr (Epi) except Coke

Depolarizing NMJ blocker

Mech: motor N blocker

Tox: hypercalc, hyperkalemia, malign hyperthermia (dantrolene)

Antidote: none during phase I (AChE-I worsen); AChE-I during phase II (repolarized but blocked)

Slective for Motor Nicotinic (ACh) receptor

Nondepol NMJ blocker (atracurium, mivacurium)

Mech: competitive (w/ ACh) Nicotinic antag

Antidote: AChE-I (neostigmine, edrophonium)

Mech: prevents Ca release from SR

Use: malignant hyperthermia tx

(caused by inhaled anesth + succinylcholine);

neuroleptic malign synd tx (antipsych drug tox)

Ergot alkaloid - potent DA Agonist

Use: Parkinson's dz

DA Ag

Use: Parkinson's dz

DA Ag (non-ergot)

Use: Parkinson's dz

(non ergots prefered)

Anti-viral/Da-releasing agent

Use: flu A, rubella; Parkinson's dz

Tox: ataxia

(anti-viral - de-coating "a man to dine takes off coat")

DA precursor

Mech: converted to DA by dopa decarboxylase

Use: Parkinson's dz

Tox: arrhythmias (d/t periph conversion); longterm use → dyskinesia w/ admin, akinesia b/w doses.

Note: use w/ carbidopa to prevent periph decarboxylation

Contra: drug-induced PD (can precipitate psychosis)

MAO-B (DA>NE) inhibitor

Mech: prevents DA breakdown

Use: adjunct to L-dopa for Parkinson's dz

Tox: enhance SE of L-dopa (dyskenesia)

COMT inhibitor (others: tolcapone)

Mech: prevents peripheral L-Dopa conversion to 3-OMD

Use: Parkinson's dz

Same rationale as carbidopa (different conversion blocked - dopa decarboxylase vs CatecholOMethylTransferase)

Anti-M ("trop/scope")

Use: Parkinsons dz (esp. drug-induced) - improves tremor/rigidity but little effect on bradykinesia

5-HT1B/1D Ag

Mech: vasoconstr; inhibs trigeminal & vasoactive peptide release

Use: acute migraine, cluster h/a

Tox: coronary vasospasm (contra: CAD, Prinzmetal's angina)

Mech: NMDA antag → prevents Ca excitotoxicity

Use: Alzheimers Dz

Tox: dizzy, confusion, halluc. (NMDA antag)

AChE-I

Use: AD

tox: nausea, dizzy, insomnia.

Local AmIde anesthetic (BupIvacaIne) Amides =2I's

Mech: 3o amines penetrate membr → become charged (locked in) → block Na chans from the inside (preferentially bind activated chan)

Use: minor surg, spinal anesth; if allergic to esters, give amides. (except coke give w/ vasoconstrictors for local)

Tox: CV tox (bupivacaine), HTN/hypoTN

Notes: 1) cannot penetrate membr in infected (acidic) tissue → req incr. dose;

2) order lost: pn- Temp- touch- Press; small /mylelinated before large/ unmyleinated(# Ca chan)

3) given w/ vasoconstr (Epi)