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115 Cards in this Set

  • Front
  • Back
Chlorpromazine
Antipsycho - Blocks D2 Receptors

high sedation and postural HT

Phenothiazine Class
Phenothiazine
Major class of Anti-Psychos

Chlorpromazine, fluphenazine, thioridazine
Fluphenazine
Antipsycho - Blocks D2 Receptors

Phenothiazine Class
Thiothixene
Anti-psycho

Thioxanthine class
Haloperidol
Anti-Psycho

high extrapyramidal effects

Butyrophenone Class

treats tourette's
Clozapine
Anti-psycho - blocks 5HT and D2

No elevated prolactin, no TD, but can cause granular cytosis = need to monitor blood. Also weight gain.
Resperidone
Anti-Psycho
Olanzapine
New gen Anti-psycho

weight gain
New gen Anti-psycos
Olanzapine
Quetiapine
ziprasidone
Aripiprazole
Tradition Anti-psyco Action
Block Alpha-Adreno/choline/dopamine/hitamine Rec.

Dry mouth, dec gastric secretion and motility

Prolactin release, weight gain, NMS
Tardive dyskenesia
Associated with Anti-psychos

hypersensitivity of Dopamine Rec. Often irreversible

use min. dose, drug holidays

Clozapine does not cause this, but has its own side effects (granular cytosis)
Tourette's Syndrome
Involuntary movements, ticks, outbursts

Haloperidol to treat
Depression
(endogenous) sadness, irritability, thoughts of death and suicide
Bipolar Disorder
Swings of mania and depression

treat with: lithium or fluoxetine+olanzapine
Mania (4 medications and type of agent)
Carbamazepine - anti-epi
Valproic Acid - anti-epi
Resperidone - anti-psycho
Arpiprazole - anti-psycho
Tricyclics

drugs names and class and common side effects
Anti-depressants

imipramine, -pramine, -triptylene, doxepine

sedation - atropine-like: dry mouth, blurred vision
CV effects: arrythmia, tachy, postural HT
Mirtazapine
tetracyclic anti-dep

alpha 2 antagonist - stimulates
CNS
Monoamine oxidase inhibitors

indication and contraindiction
MAO Inhib. anti-depressant

Tyramine in diet along with MAOS = HT
Tranylcypromine
MAO inhbitor - similar to amphetamine, reversible
Phenelzine
MAO irev. inhibitor
isocarboxazid
Rev MAO inhibitor
Selegiline
Path form MAO inhibitor
SSRIs

3 drugs
selective serotonin reuptake inhib.

Anti-deps

Fluoxetine - prozac
Paroxetine - paxil
Sertraline - zoloft

approved for addicition, bulimia, alcholism
Beyond SSRIs

3 drugs
venlaflaxine
duloxetine = block nor epi and serotonin reuptake

st johns wort - herbal remedy under trial
OCD Treatment
SSRIs

Fluoxetine
Paroxetine
Sertraline
Generalized Anxiety Disorder

Characteristics and 3 drugs of choice
GAD - irritability, muscle tension, autonomic arousal,

Alprazolam (benzodiazepine), most common
paroxetine - paxil - antidep - 5HT
vanlaflaxen - "beyond SSRI" - both norepi and 5HT
Panic Attacks
Symptoms and drugs
Anxiety
Fear, chest pain, tachy, sweating, breathing, swallowing

alprazolam, sertraline, paroxetine, vanlaflaxin
Benzo Metabolism
Benzodiazepine to nordiazepam to oxazepam
Flumazenil
Benzo antagonist - antidote
Beta-carboline
inverse antagonists of benzos, bind same rec. but elicit opposite response, convulsions/tension
Benzo Theraputic Uses
Anxiolytics
anticonvulsants - clonazepam
muscle relaxants - diazepam
sedative - IV diazepam, trilazam
withdrawl - diazepam
Buspirone
No CNS depression
Treat GAD
non-benzo
Epilepsy

Characterize
convulsions caused by irregular firing of nerves

Imbalance between NMDA and GABA

to treat: decrease NMDA, increase GABA
Epi Seizer types:

Partial
Simple: older child, adults: no conscious impairment

complex: older children/adults: some conscious impairment
Epi Seizer types:

Generalized
absence - 4-8yr - partial loss consciousness throughout day

tonic-clonic- all ages - jerking, falling spasms

infantile - 4-9months - flexure, convulsions, death
Infantile spasms

Treatment
Vigabatrin - increases GABA in brain, inhibits GABA aminotransferase

Causes loss of vision

ACTH approved - unknown mechanism
Main mechanisms for anti-epi drugs

Three mech. with drugs examples
1) promote inactivate stated of voltage Na channels (carbamazepine, phenytoin)

2) GABA mediated synaptic inhibition (barbs and benzos)

3) limit activation of T current (Ca volt chan) (ethosuximide)

Multiple drug therapy for multi types of seizures
Metrazole Tests
Test given to animal subjects to induce absence seizure.

block with ethosuximide or sodium valproate
Maximal electroshock test
Tonic-clonic type seizure induced in mice with shock.

block with carbamazepine or phenytoin
Phenobarbital
Anti-epi - Used against partial seizures and tonic-clonic seizures

Increases GABA
Induces liver P450 enzyeme act.
Phenytoin
Anti-Epi
all forms except absence

no sedative effect
blocks Na chan
gingival hyperplasia, nystagmus
Fosphenytoin
Anti-epi -
Phenytoin prodrug - metabolized to active form by blood phosphates
Carbamazepine
Anti-epi
all except absence

blocks Na chan
Vs. trigeminal neuralgia
double vision/dizzy/ataxia
ethosuxamide
Anti-epi
drug for absence seizures

Reduces Ca chan conductance in thalamus

dizzy/ataxia/nausea
Valproic/dipropylacetic acid
Anti epi-
blocks tonic-clonic and partial primarily
secondary drug for absence

Na chan and increase GABA

liver failure, pancreatitis, not for preggers
clonazapam
Anti-epi Benzo

absence seizures if no others work

facilitates GABA

sedation/drowsiness
Status epilepticus
continued state of epilepsy

lorazepam IV - a benzo
Gabapentin and Lamotrigene and pregabalin
add on drug for adult partial seizures
Topiramate
Partial and tonic-clonic seizures
migranes

weight loss, dizzy, hyperthermia
Sedative/Hypnotics

General Characteristics
Sedative - tranquillize
Hypnotic - induce sleep

same drugs work along continuum

benzos and barbs
Barbiturates
extend along entire continuum from wakefulness to death (anesthesia and coma)

use is restricted

increase duration of cl- chan opening

does induce P450 in liver, increases metabolism of other drugs

GABA mimetic
Benzodiazepines
Most common sedative-hypnotic

does not extend into anesthesia/coma/death end of spectrum

increases frequency of Cl- chan opening

do not induce P450 enzymes in liver

not GABA mimetic
Hypnotics and GABA
Both benzos and barbs act on GABAa ionophore, which regulates Cl- ions into the cell

Different variations of the ionophore exist throughout the body, benzos and barbs act on different variations
Benzo Receptor Agonists
Agonists:triozalam, diazepam
trad. benzo drugs for sedation
activate gaba - Cl- enters cell - supressed
Benzo Receptor Antagonists
flumazenil - imidazodiazepine
blocks benzo but not other sedatives - wake up instantly

diazepam binding inhibitor
blocks benzo at receptor
Benzo inverse agonist
beta-carboline - binds benzo receptor but causes stimulation (opposite response)
Benzo application
wide use- anti anxiety, anti-epi, sedative
because of
different distribution throughout the brain
Triazolam
sleep inducer
zolpidem and eszopiclone
sleep inducers, bind benzo rec but are structurally unrelated to benzo. faster peak activity. can use for longer period of time.
Parkinsons disease symptoms
tremor at rest
rigidity
bradikinesia
postural instability

extrapyramidal component effected
PD patho
extrapyramidal system
4 neurotransmitters: DOPA and ACH (gaba and gluta)

loss of dopamine secreting cells
Iatrogenic PD
haloperidol, phenothiazine - block DA Rec
Primary Goals of Anesthesia
preserve px life
provide good surgical field
block pain
Balanced Anesthesia
combination of drugs are used for best results and least side effects
Nuroleptanesthesia
combo of anti-psyco and analgesic

analgesia with amnesia

px drowsy but awake
Dissociative Amnesia
ketamine

catonia, amnesia, analgesia
MAC
minimum alveolar concentration

minimum amount of drug needed in lungs to produce no response from surgical stimulus on 50% of patients

lower the MAC the more potent the drug
stages of anesthesia
stage 1 - analgesic, conscious
stage 2 - delirium - not good, go past
stage 3 - surgery, substages, good
stage 4 - medullary paralysis - death - not good
Sites of general anesthesia

by stage
1 - substantia geletinosa
2- inhibitory neurons
3- brain stem - reticular formation
4 - medulla
Meyer-overton
Theorized that anesthetic potency was based solely on lipid solubility

was incorrect
blood gas partition Coef.
PC = molar conc. in blood / molar conc in lungs

lower the PC the faster it will induce anesthesia
second gas effect
if two gasses are given one at a higher concentration the second gas will enter at a faster rate than if given alone. the first gas essentially pulls the second one along with it
anesthesia pharmokinetics

summarize 4 main points
1) lower PC = faster induction
2) rate of induction is not related to MAC
3)increased ventilation yields faster induction
4)in combo, higher concentration gases can pull lower concentration at a higher rate than if alone
Anesthesia effects on main systems
all exclude N2O
CVS: dec. mean arterial BP
Resp: depress TV, increase rate = depress Resp.
Liver: low, except halothane
kidney: low effect
skeletal muscle: relax
smooth muscle: relax, no preggers, only N2O
Advantages to using Anesthesia Gas
easily change blood concentration by changing gas concentration mix
Nitrous oxide

properties
excreted through lungs, no liver metabolism

fast onset, fast recovery

low potency

sedative, analgesic

not used long term

alone - sedative analgesic
full anesthesia used as adjunct

very slight effect to body systems

side effects
short term: hypoxia, can pull O2 out with it, give with O2
long term: bone marrow
possible risks with fertility
Nitrous Abuse
death by asphyxiation

long term abuse: brain damage, verbal memory loss
halothane
20% liver metabolism, too high.
poor kinetics, very soluble

used to be used on children b/c can be used with mask induction.

hypatotoxicity, malignant hyperthem, arrythmia

cheap
malignant hyperthermia
caused by halothane

dantrolene to treat
enflurane
not used. causes seizures.
isoflurane
most commonly used in US. not as good with children. no harmful side effects known.
desflurane
rapid induction rapid recovery, faster than isoflurane

irritates airways, no mask induction
sevoflurane
high metabolites, but no indication of liver/kidney damage

mask induction, replacing halothane for children

interracts with soda lime in rebreather, toxic. use fresh gas no rebreathing.
CVS and anesthesia
desflurane and isoflurane have least effect on Cardiac Output

all suppress BP
IV anesthesia
lower cost, rapid onset

harder to lower conc, therefore shorter acting

lipophillic -> brain and spinal cord

can infuse into fat and leach out later with effect
Ultra-Short acting barbs
thiopental and methohexital

prolonged use leads to grogginess

dec. cerebral metabolism

hypotension, depressed resp, laryngospams
propofol
better maintenance drug, better recovery,

hypotension, no grogginess
etomidate
used for induction only

terrible side effects
death, myclonic movement, painful, nausea, vomitting,

less resp and cardio depression
ketamine
PCP

dissociate anesthesia - catatonic

increases CVS: HR, CO, BP
increases intracranial pressue

cardiac patients

hallucinations
Anesthetis adjuncts:

benzos
diazepam/lorazepam - long acting

midazolam - short acting

sedation, reduce anx, amnesia
Anesthetis adjuncts:

opiods
anagesia

morphine - long acting
remifentanil - shortest

can give full anesthesia

prolonged resp. depression - stone chest
Cocaine
first local anesthetic
local anesthetic chem structure
1) lipophilic group
2)amide or ester
3) hydrophilic group
Local anesthetic esters
cocaine
procaine
chloroprocaine
tetracaine
proparacaine benzocaine

Esters don't have an I before the "caine"
Local anesthetic amides
All have an I before the "caine"

lidocaine
mepivacaine
prilocaine
etc
Ethers
local anesthetics

pramoxine - hemmeroid
phenacaine - ophthalmology
dyclonine
ketone and ether local anesthetic

sucrets, throat lozenge and spray
pH and local anesthetic
cationic acid to neutral base

non-ionic form penetrates membranes
ionic form binds mote actively
pH Effects
usually local anesthetic will come as salt in HCl or in carbonated solution
Absorption of local anesthetic
not important - can be toxic

given with epi as vasoconstrictor to minimize absorption
Uses for muscarinic Agonists
eye surgery
glaucoma
non-obs atony of bladder
paralytic ileus
xerostomia
dx asthma
examples of muscarinic agonists
Ach
bethanechol
carbachol

muscarine
pilocarpine
muscarine
toxic ingestion from mushroom

ab cramps, GI stimulation, excess secretion
pilocarpine
muscarinic/cholinergic agonist

xerostomia, glaucoma
contraindications for musc. agonists
asthma
hyperthyroidism
peptic ulceration
cholinesterase inhibitors

uses
prevent hydrolysis of Ach

-stigmine and edrophonium

paralytic ilieum
glaucoma
myasthenia gravis
reverse nuromusc blockade
antimuscarinic toxication
alzheimers - donepezil/rivastigmine
organophosphates
irrev cholinesterase inhibitors

echothiophate - glaucoma
malathion/parathion - agg pesticide
soman/sarin - war chemical

antidotes: atropine, lorazepam pralidoxime
scopolamine
cholinergic antagonist

prevents motion sickness
benztropine
cholinergic antagonist

reverses symptoms of iatrogenic PD
dicyclomine, glycopyrrolate
cholinergic antagonist

dec. GI sec, motility, spasm
Oxybutynin, tolterodine
Darifenacin, solifenacin
cholinergic antagonists

decrease mituration
dec bladder spasms
Ipratropium
Tiotropium
cholinergic antagonists

dec. broncial spasm and sec.
how to increase increase elimination via urine
weak acid - make urine alkaline
weak base - make urine acidic
steroid hormone signaling
activation of intracellular receptor then binding to DNA
muscarinic receptor blockers useful for
mydriasis and cycloplegia for eye exams