Midterm Reviewer

Central Nervous System

Analgesics A. Narcotics-dull sense of pain and cause drowsiness or
A. Narcotics and sleep
Opiods -relieving severe pain and preoperatively to reduce
B. NSAIDs anxiety and induce anesthesia
-can supress the ability to breathe and cause coma and
death
• Morphine
• Codeine
• Oxycodone
• Hydromophone
• Meperadine
• Tramadol-inhibits reuptake of norephonephrine
and serotonin
-bind to mu opiod receptors
• Fentanyl-conscious sedation and breakthrough
for cancer pain
-100 times more potent than morphine
-administred with benzodiazepine for preoperative
pain control and anesthesia
-transdermal
-slowly absorbed 48-72 hours
• Methadone
B. Non-Opiod
C. NSAIDs- not to be taken with heparin or warfarin
• Aspirin-only NSAID able to irreversibly inhibit
COX-1
-inhibition of platelet aggregation
• Indomethacin
• Diclofenac
• Ibruprofen-minimizes prostaglandins
-less irritnat to the esophangeal and gastric linings
• Mefenamic Acid
• Meloxicam
• Celocoxicab-block COX-2
• Naproxen-headaches and menstrual pain
-anti-inflammtory, arthritis, sprains and
inflammation-based pains
-administered every 8-12 hours
• Ketoralac-very potent NSAIDs
-both inflammtory and non-inflammatory pain
- not used for more than 5 days
-adverse effects on kidney and cause ulcers
 • Acetaminophen- analgesic and antipyretic (not
anti-inflammatory)
-blocks pain peripherally
-milder effects on upper digestive tract
-OD: renal failure or hepatic toxicity
-safer choice for hemophiliacs, patient taking
blood thinners and for children
-first line of defense for headaches, muscle aches,
arthritis, backache, toothaches, colds, and fevers

Seizure Disorder and • Hydantoins

Epilepsy • Long-acting Barbuturates
• Succinamides
• Benzodiazepinnes
• Carbamazepine
• Valproate (Valporic Acid)
Anticonvulsants • Carbamazempine
• Gabapentin-treatpartial seizures and neuropathic pain
• Topiramate
• Valporic Acid-manic episodes, Bipolar Disorder,
Schizophrenia, Tardive Dyskinesia, Agression, ADHD
-increase GABA concentrations and blocks voltage-gated
sodium channels and T-type calcium channels
-alternative to lithium salts
• Phenobarbital-sedative hypnotic
-enables binding to inhibitory GABA subtype receptors
-elevates seizure threshold and redeuce spread of seizure
activity
-inhibits calcium channels and decrease stimulative
transmitter release
• Levetiracetam-monotherapy in partial seizures
-treats neurpathic pain
-binds to a synaptic vesicle glycoproteins, SV2A to
inhibit the abnormal spread of signals
• Phenytoin-used for generalized tonic-clonic (grand mal),
complex partial seizures and status epilepticus and Bell’s
palse
-inhibits spread and frequency of seizures by altering ion
transport; sodium channels
-stabilize the threshold against hyper-excitability caused
by excessive stimulation
-“high priority” alarming at higher doses
-gingival enlargement, Steven Johnson’s syndrome, and
toxic epidermal necrolysis, increased risk of suicide
-first line of defense for epilepsy
 • Benzodiazepines-anticonvulsants, muscle relaxants,
sedatives, and hypnotics
-enhance the response to the inhibitory neurotransmitter
GABA by opening GABA-activated chloride ions to
enter the neuron
Parkinson’s Disease- • Carbidopa-Levodopa-crosses the blood brain barrier
dopamine die or become and converted to dopamine
damaged -most effective for use in PD
-metaboli precursor of dopamine
Treatments: Either -discoloration of saliva, urine, sweat may occur
increases dopamine or -Neurolepltic malignant syndrome
attacks acetylcholine to -overdose (gastric lavage, IV fluids, and satisfactory
balance out the airway maintained)
concentrations -limit protein as it decreases drug absorption
-do not initiate until monoamine oxidase inhibitor have
been discontinued for a minimum of 2 weeks
• Pramipexole
• Ropinirole-acts as a dopamine receptor
-avoided in pregancy, dysrythmias, cardiac disease,
hepatic and renal disease, psychosis and affective
disorder
-sleep attacks and narcolepsy
-taken with meals
-therapeutic effects may be seen in weeks to a few
months
• Seligine (Monoamine Oxidase B(MAO-B) inihibitor)
• Entacapone (COMT inhibitor)
• Benzatropine (anticholinergics)-blocks acetylcholine to
balance with dopamine
-diminish involuntary movements
-OD (gastric lavage and Physostigmine)
-should be taken at the same time of the day
-not taken with CNS depressants
-susceptible to heat stroke
-not to drive or operate machineries
• Amantadine (anticholinergics)causes release of
dopamine in the neurons rebalancing acetylcholine
-prophalaxis or treatment of influenza
-monitor input and output
-livedo reticularis (mottling of skin, lower extremity
edema nd pruritus)
-after meals for better absorption and decrease GI
symptoms or atleast 4 hours before bedtime to prevent
insomia
Alzheimer’s Disease-loss Cholinesterase inhibitors-curb breakdown of acetylcholine to
of memory and other increase acetylcholine concentrations
intellectual abilitis • Donepezil-approved for all stages of AD
-altered acetylcholine, -vagatonic effects(lead to bradycardia and complete heart
glutamatem and other block)
neurotransmitters • Galantamine
concentraions and its • Memantine (moderate to severe AD)-NMDA receptor
effectiveness antagonist
-prevents destructive chain of events
-may cause Steven-Johnson’s syndrome
-administer with a glass full of water
-larger than 5 mg then should be divided into two doses
• Rivastigmine

Amyotrophic Lateral • Riluzole-anti-glutamate agent

Sclerosis-rapidly -inhibitory effect on glutamate release, inacivatin of
progressive weakness, voltage-dependent sodium channels
muscle atrophy, -track liver function
fasciculations, muscle -give one hour before or two hours after meal
spasticity, difficulty -avoid high fat diet (decreases drug absorption)
swallowing, breathing, and
speaking

-death of both upper and

ower motor neurons in the
motor cortex of the brain
Muscle Relaxants -seek to Neuromuscular Blockers-prevents nueromuscular transmission
ease painful and at the neuromuscular junction, causing paralysis of the affected
involuntary contraction of skeletal muscles
injured or overstimulated
muscle cells Spasmolytics / Antispasmodics-centrally-acting, blocks
-treat muscle spasms and intraneuronal pathways in the spinal cord and in the midbrain
spasticity reticular activating system
• Carisprodol-depress the CNS
Mucle Spasms- sudden -sedation and alteration in pain perception
invluntary contractions of • Methacarbamol-centrally acting
one and more muscle -depress in the spinal cord resulting to muscoskeletal
groups realaxation
• Baclofen-centrally acting
Spasticity-state of -blocks the activity of the nerves within the part of the
increases muscular tone brain that controls contractions and relaxation
with amplification of the • Diazepam-centrally acting
tendon reflexes -antianxiety, antidepressant and skeletal msucle relaxant
-heightens the actions of GABA
-anxiety, alcohol withdrawal, seizure disorders
 -smoking decreases effect by increasing rate of
metabolism
• Dantrolene-centrally acting
-prevents intracellular realease of calcium from
sarcoplasmic reticulum
• Cyclobenzaprine-increase stage 4 sleep, beneficial for
patients suffering with fibromyalgia
-increased norephinephrine release
-used for fibrpmyalgia

Side Effects
• Dizziness,dorwsiness, headache, tremor, depression,
postral hypertension, tachycardia, nausea and vomiting,
urinary retention, diplopia, seizures

Contraindications
• Pregnancy, breastfeeding, geriatric patients, renal/hepatic
disease, addictive personality disorders, myastenia gravis
and epilepsy

Local Anesthetics- for • Procaine(Novocain)-reduce the pain intramuscular

pain not controlled using injection of pennicillin
oral medications or other -inhibits sodium influx through volatage-gated sodium
types of medications channels
-dentistry
• Lidocaine-local anesthetic and cardiac depressant
-inhibits ionic fluxes required for the initiation and
conduction of impulses
-relieves itching, burning, and pain from skin
inflammation
-denta anesthetic for minor surgery
• Benzonatate-peripherally acting
-non-narcotoc oral cough suppresant and antitussive
-decreases sensitivity of stretch receptors in the lower
airway and lung
 Autonomic Nervous System
Adrenergic Agonist Drugs Non-selective agents-act on particular adrenergic
(Sympathomimetic Drugs) receptors anywhere in the body
-mimics Sympathetic responses of
the body • Epinephrine-direct-acting adrenergic agonist that
• Dilation of pupils stimulates all alpha and beta adrenergic receptors
• Inhibit salivation -potent cardiac stimulant that increases
• Dilate brinchi contractility and heart rate by beta1 receptor
• Accelerates heartbeat stimulation
• Inhibits digestion -causes contraction of vascular smooth muscles
• Stimulates glucose release -vasoconstriction (leads to higher BP to
• Stimulates epinephrine compensate for low blood volume)
and norephinephrine -relaxation of respiratory and uterine smooth
release muscle
-used for circulatory support and treatment of
• Inhibits peristalsis and
airways swelling in severe acute anaphylactic
secretion
reactions and shock
• Relaxes bladder
-return circulation in cardiac arrest during
cardiopulmonary resuscitation
-short-acting and source of the allergic reaction
may still be present after the drug is metabolized
• Norephinephrine- potent vasopressor and cardiac
stimullant
-little impact on Beta2 receptors (lungs and
airway)
• Ephedrine- acts on cardiac stimulation,
bronchodilation, and vasoconstriction
-produces mild stimulatory effects (useful for
narcolepsy and depression)
-abuse for athletic performance enhancer and
appetite suppresant
-decrease urine formation
• Dopamine-potent vasoactive agent
-dopaminergic and beta1 adrenergic effects
-increase renal and splanchnic blood flow and
increased cardiac contractility
-immediate precursor of norephinephrine
-shock states, low cardiac output syndromes,
hypotension, to increase cardiac output and blood
pressure
-Dopamine extravasation can cause tissue
sloughing and necrosis (should be infiltrated
immediately with 10-15 ml nomal saline with 5-
10 mg of phentolamine)
 Selective Adrenergic Agonists- act pn adrenergic
receptors in specific, taergeted locations
• Dobutamine-used for depressed cardiac
contractility, cardiac surgical interventions, acute
myocaridal formations
-treat low carodac output following cardiac arrest
-Beta1 adrenergic receptors
-increased effects with antidepressants
• Phenylephrine- potent synthetic vasopressor that
acts on alpha1 receptors to produce
vasoconstriction
-topical properties reliece nasal congestion from
allergic conditions or common cold
-used for decongestant properties
-hemorrhoids and anti-swelling properties
-precippitation of hypertensive crisis
• Clonidine-selective alpha2 agonists
-antihypertensive and central analgesic
-produces a reduction in hear rate by inhibition of
cardioaccelerator activity in the brain
-Alpha2 inhibits production of norephinephrine
(decreased norephinephrine results to lower blood
pressure)
• Dexmedetomidine-selective alpha2 agonist
-sedatives, anxiolytic, and analgesic effects
-supress the firing of noradrenergic neurons
-primarily for hypotension and bradycardia
Adrenergic Antagonist • Yohimbine- treatment of erectile dysfunction
(Sympatholytic) • Phenoxybenzamine-nonselective alpha-
-blocks normal sympathetic adrenergic antagonist
responses of the body; block -blocks the effects of norephinephrine and
binding sites epinephrine
-irreversibly binds to receptors and new receptors
must be synthesized for the termination of effects
of this drug
-Vasopressin may correct hypotension due to
administration of phenoxybenzamine
• Phentolamine
-competitive, nonselective alpha-receptor
antagonist
-reversible and drug effects can overcome by
increasing concentrations of an alpha-receptor
agonist
• Prazosin- selective, alpha1 receptor antagonist
-decreases smooth muscle contraction
-treats hypertension
 -increases the concentration of high density
lipoproteins and decreases the concetration of
low-density lipoproteins
• Terazosin-less potent, longer acting analog of
prazosin
-used primarily in the management of benign
prostatic hyperplasia
Beta-Adrenergic Antagonists – Beta1 Receptor Antagonist-decreased heart rate and
block effects of agonists myocardial contractility
(norephinephrine and Beta2 Receptor Antagonist-inhibition of vascular dilation
epinephrine) and inhibition of pulmunary brionchiole dilation
-prevents cardiac and pulmonary
excititation • Propanolol-both beta1 and beta2 receptors
-management of tremor, thyroid storm, nad
pheochromocytoma
-interacts with warfarin
• Metraprolol- B1 receptor
-limiting heart rate ,hypertension
• Esmolol-B1 receptor antagonist
• Atenolol- B1 receptor antagonist
-elimintaed unchanged in the urine, risk for OD in
patients with impaired renal functions
• Nadolol-nonselective; long half-life; allowing
once a day dosage
• Pindolol-nonselective
-weak beta receptors
• Labetalol-decreases blood pressure without
compensatory increase in heart rate; hypertension
• Carvedilol-Alpha1, Beta1, Beta2 adrenergic
receptors
-antioxidant and antiproliferative properties
-chronic heart failure and postmyocardial
infarction

Avoid postural hypotension

• Dangle legs for a few minutes
• Rise slowly and stand for a moment
• Move slowly and do not change position readily
Directly Acting Acetylcholine • Bethanechol--stimulates muscarinic receptors on
Receptor Agonist the bladder, causing contraction and urination
(Parasympatomimetic) -peristalsis; causing defacation
-postpartum and postoperative unobstructed
urinary retention
 Acetylcholinesterase Inhibitors • Neostigmine- myasthenia gravis
-block metabolic effects of the -treat urinary retention and paralytic ileus
enzyme acetylcholinesterase -antidote for nondepolarizing skeletal
-allows acetylcholine to relaxants(paralytic agents)
accumulate in synapses and • Physotigmine- myasthenia gravis
subsequently increases -treatment of central toxic effects of atropine and
acetylcholine receptor stimulation scopolamine
-PNS effects predominate due to -only anticholinesterase drug that crosses the
increased acetylcholine activity at blood-brain barrier in an intact form
muscarinic sites • Edrophonium- short acting cholinergic
-life support equipment such as atropine(antidote),
endotrcheal tubes, oxygen, and ventilators should
be available
• Pyridostigmine- similar with neostigmine
-maintenance drugs for myasthenia gravis
-long duration of action
-effective for 8-12 hours
• Donepezil-acetylcholine is not metabolized
quickly
Cholinergic Antagonists • Atropine- short duration of action
(Parasympatolytics) -treat excessive cholinergic stimulation caussed by
-blocks the action of acetylcholine anticholinesterase toxicity, mushroom poisioning,
-decrease respiratory and nerve gases, organophosphate pesticide poisoning
gastrointestinal secretions • Glycopyrrolate-increases heart rateand
-prevent drop heart rate caused by bloodpressure to a lesser extent than atropine
vagal intubation during intubation • Scopolamine – mydriasis
-OD treated with physotigmine
• Ipratropium- inhalation treatment for COPD to
produce bronchodilation
-used as nasal spray to relieve rhinorrhea
• Tiotropium Bromide-long-acting antimuscarinic
anticholinergic to produce bronchodilation
-daily maintenance for patients with COPD
• Benztropine- centrally-acting anticholinergic
drug
-decrease symptoms of PD
• Oxybutynin- increases bladder capacity and
decreases voiding frequency