"1st generation" H-1 Blockers

many drugs, many OTC, many found in multi-ingredient cough/flu/cold remedies

Strong atropine-like actions

Sedating

Good local anesthetic activity

Uses:

Relief of mild allergy S/Sx

Sedative/hypnotic

MANAGEMENT OF PARKINSON'S 

SE/CI/OD

Same as atropine...

Fexofenadine (Allegra)

Loratadine (Claritin)

Desloratadine (Clarinex)

Cetrizine (Zyrtec)

Basically no atropine-like SE/CI

not sedating

OK for asthma

Cimetidine (Tagamet)

Ranitidine (Zantac)

Nizatidine (Axid)

Famotidine (Pepcid)

Cimetidine is most widely used example of a drug that causes DDI

Corticosteroids

(Glucocorticoids)

The "cornerstone" of tx

decrease inflammation

AREN'T BRONCHODILATORS

"restore" sympathomimetic efficacy thats lost when its needed most

Beclomethasone (Vanceril)

Orally inhaled steroids

minimal systemic absorption, so minimal systemic effects

local (airway) anti-inflammatory actions

prophylaxis ONLY

used alone or with other drug, depending on asthma frequency, severity

SE:

hoarseness, cough, thrush

Problems with compliance because doesn't work right away

Montelukast (Singulair)

Block LT receptors, "interrupt" various inflammatory processes including bronchoconstriction, inflammatory cell migration, local edema

For CONTROL treatment ONLY 

"modestly effective"

Albuterol (Proventil)

Sympathomimetic Drug

"selective" B-2 agonist

airway action:

brochodiliation

NO anti-inflammatory activity

Salmeterol (Serevent)

B-2 agonist with slow onset, long duration vs. albuterol and most others

control med only

NOT suitable for rescue

NOT a substitute or replacement for corticosteroids

Methylxanthines

Prototype: Theophylline

Same group as caffine

VERY LOW MARGIN OF SAFETY

must normalize dose to body wt

common drugs interact to alter metabolism, half-life, blood levels

SE:

CNS stimulation

CV Stimulation

Antimuscarinincs for asthma therapy

decrease ACh-mediated bronchoconstriction

Slight decrease of ACh-mediated mucus hypersecretion, but mucus becomes VERY thick, cruddy

atropine: inhaled, for status asthmaticus

Lidocaine (Xylocaine)

Amide 

most widely used, overall, of all LAs

closest to "ideal"

metabolically inactivated in liver

NAME RECOGNITION: if a drug's generic name ends in "caine" and the letter "i" appears twice in the generic name, its an amide-type LA!

Procaine (Novacain)

Seldom used; properties are far from ideal

not very potent, slow onset of action and short duration of action

NAME RECOGNITION: "I" appears only once in generic name

Ester

used topically

powerful cerebral cortical stimulant

has sympathomimetic activity on its own

Main ingredient in OTC local anesthetic products, esp for use on skin

ester

structure, properties prevent good diffusion into nerves

*numbing agent in dental work before shot

new and now most widely used antidepressant class

certain advantages over older agents

until not too long ago, main class for depression tx

still used because of cost

Fluoxetine (Prozac)

Sertraline (Zoloft)

Citalopram (Celexa)

Escitalopram (Lexapro)

Paroxetine (Paxil)

Fluvoamine (Luvox)

Selective Serotonin Re-uptake Inhibitors (SSRIs)

main antidepressant effect due to selective decrease of serotonin reuptake by certain brain neurons which causes an increase in the postsynaptic neurotransmitter (serotonin) levels and postsynaptic effects which cause decreased symptoms

Imipramine (Tofranil)

Tricyclic Antidepressant

a large group of older generation antidepressants that are being used less since introduction of SSRIs but are still used mainly because of cost

seem to decrease depression signs and symptoms by decreasesing neuronal reuptake of all the main biogenic amines: DA, NE, seratonin

inhibit metabolic inactivation of NE, Dopamine, serotonin

ONLY FOR SEVERE, REFRACTORY DEPRESSENT

LIMITATIONS: hypotension; hypertensive crisis from interaction with common foods, medications that contain mixed- or indirect-acting sympathomimetic, or food/beverages with tyramine; interaction with any drug w/ atropine-like actions

"low potency" 

major class of antipsychotics

block dopamine, ACh, histamine, and alpha-adrenergic receptors in CNS and in periphery

extrapyramidal side effects (EPS)

"high potency" 

fast onset, short acting

greater risk of EPS

fewer/milder autonomic SE

lowers seizure threshold

Clozapine (CLOZARIL)

block serotonin receptors

weak DA receptor blockade (very low incidence of EPS)

few peripheral autonomic SE

decreased WBC count, increased risk of infection

Levadopa (L-DOPA, LARODOPA, DOPAR)

Body's natural precursor of DA

two main sites of L-DOPA metabolism: Gut and Brain

DA formed outside of brain CANNOT cross BBB

for all causes of parkinson's except drug induced

severe PD or PD that doesn't respond well to DA agonists

Selegiline (ELDEPRYL)

"selective" MAO-B inhibitor for PD

"preserves" DA in EPS neurons by decreasing metabolic inactivation of DA by MAO

Adjunct to Levodopa for advanced PD

"Trihexphenidyl (ARTANE)

Benztopine (COGENTIN)

Diphenhydramine (BENADRYL)

"centrally-acting" antimuscarinics

blocks central ACh muscarinic receptors

Carbamazepine (TEGRETOL)

Phenytoin (DILANTIN)

Valproic Acid (DEPAKENE)

Schedule II

absorbed well from all injection sites

poor bioavailability orally

analgesia:suppression of pain

best for moderate to severe pain; decreased pain sensation plus euphoria 

cause sedation

ventilatory depression

decreased GI motility 

Naloxone (NARCAN)

cancels opiods

duration of action << that of the agonist, so repeated doses is almost always necessary 

may cause acute withdrawal in opioid-dependent person

Meperidine (DEMEROL)

lesser effects on gut, biliary tract, bladder, uterus vs most opioids.

overused

possibly fatal reaction with MAO inhibitors

analgesic efficacy about same as aspirin/acetaminophen (not for severe pain)

efficacy enhanced by aspirin/acetaminophen

people can crush OXYCONTIN extended release tablets to "get high quicker"

injected, potency about same as morphine

better oral bioavailability

long duration of action

use in opioid detox or maintenance programs

propxyphene (DARVON)

very low analgesic efficacy 

marginally better if combined with aspirin or acetaminophen

OD: toxic psychosis 

Pentazocine (TALWIN)

"partial opioid agonist"

weak agonist (analgesic) when given alone

blocks mu receptors for more efficacious opioids

can decrease cardiac output

GHB (Gamma Hydroxybutyrate)

Crosses BBB, s metabolized into GABA which causes CNS depression

"date rape drug"

Diazepam (VALIUM)

Lorazepam (ATIVAN)

Benzodiazepine

main class of CNS depressants

Flumazenil (ROMAZICON)

specific antagonist at benzodiazepine receptors

used to diagnose or treat known or suspected OD of a benzodiazepine

Has no effects on receptors for other drugs

Flunitrazepam (ROHYPNOL)

"Roofies"

"date-rape drug"

10x potency of diazepam

causes "typical" benzo effects including amnesia, and effects are dramatically intensified by alcohol

Dextroamphetamine (DEXEDRINE)

Amphetamine mixture (ADDERALL)

Methylphenidate (RITALIN)