MODULE 6 Anesthetic Agents Adverse and Side Effects

general: headache, extended somnolence, delirium, hypotension,

Anesthetics arrythmias, shock, decreased cardiac output, acidosis, hiccups, nausea,
-drugs that are used to cause complete or partial loss of sensation* vomiting, kidney damage, bronchospasm, laryngospasm, apnea, cough,
-general anesthetics are able to produce amnesia**, analgesia, and malignant hyperthermia
unconsciousness by creating widespread depression in the CNS; given local: tremors, dizziness, headache, restlessness, anxiety, arrhythmias, hyper
parenterally or by inhalation or hypotension, peripheral vasodilation, cardiac arrest, blurred vision,
-local anesthetics are able to block sensation in a specific area of the body; nausea, vomiting, respiratory arrest
methods include topical, infiltration, field block, nerve block and IV regional
anesthesia. General Anesthetics
Prototype Drug Related Drugs Drug Classification hypersensitivity, status asthmaticus, pregnancy*, lactation, cautious use in
thiopental droperidol, etomidate, parenteral general cardiac disease, shock, hypotension, increased ICP, myasthenia gravis
ketamine, anesthetics
methohexital, Local Anesthetics
midazolam, propofol hypersensitivity, shock, heart block, pregnancy**, lactation, cautious use in
halothane enflurane, isoflurane, inhalation general CHF, respiratory depression, renal and kidney disease, shock, elderly, and
nitrous oxide anesthetics familial history of malignant hyperthermia
lidocaine benzocaine, local anesthetics
bupivacaine, General Anesthetics
chloroprocaine, IV solution must be prepared just before the administration and given
dibucaine, immediately
levobupivacaine, assess vital signs before, during, and after administration
pramoxine, procaine, provide emotional support preoperatively
ropivacaine administer preoperative medications on time
monitor for nausea and vomiting, and institute appropriate measures to
Balanced Anesthesia prevent aspiration
pre-operative medications: may include use of anticholinergics that assess postoperative pain and administer
decrease secretions to facilitate intubation and prevent bradycardia analgesics
associated with neural depression
sedative-hypnotics: relax the patient, facilitate amnesia, and decrease Local Anesthetics
sympathetic stimulation topical preparation must be kept out of eyes
antiemetics: decrease the nausea and vomiting associated with the slowing no topical administration to injured skin
of GI activity lidocaine (Xylocaine) solution containing preservatives cannot be given for
antihistamines: decrease the chance of allergic spinal or epidural block
reaction and help to dry up secretions assess vital signs before, during, and after
narcotics: aid analgesia and sedation administration
emergency equipment must be available during administration
Administration of General Anesthesia
stage 1 (analgesia stage): loss of pain sensation, with the patient still MODULE 6: Central and Peripheral Nervous System Drugs
conscious and able to communicate
stage 2 (excitement stage): period of excitement and often combative Muscle Relaxants
behavior, with many signs of sympathetic stimulation** • relieve musculoskeletal pain or spasm and
stage 3 (surgical anesthesia): involves relaxation of skeletal muscles, return of severe musculoskeletal spasticity
regular respirations, and progressive loss of eye reflexes and pupil dilation; • used to treat acute, painful musculoskeletal
surgery can be safely performed conditions and muscle spasticity associated with
stage 4 (medullary paralysis): deep CNS depression with loss of respiratory Multiple Sclerosis (MS), cerebral palsy, stroke,
and vasomotor center stimuli, in which death can occur rapidly and spinal cord injuries
• 2 main classes
Anesthetics Client Teaching • centrally-acting
General Anesthetics • peripherally-acting
-the nurse should perform standard preoperative teaching
alleviate anxiety, and answer patient’s questions Centrally-Acting
-consciousness is lost quickly • acts on the central nervous system
Local Anesthetics • used to treat acute spasms caused by anxiety,
-the nurse should perform standard preoperative teaching, inflammation, pain and trauma
alleviate anxiety, and answer patient’s questions • a patient with acute muscle spasms may receive
-report confusion, pain in injection site, faintness, and/or heart palpitations one of the following drugs
-as drug takes effect, the senses will be lost in the following order: • baclofen
temperature, pain, touch, position sense, and muscle tone • carisoprodol
• chlorphenesin
Pharmacodynamics • chlorzoxazone
general: the exact action is not known but these drugs are able to reduce the • cyclobenzaprine
activity of the cerebral cortex and the reticular activating system • metaxalone
local: interfere with the initiation and conduction of impulses in nerve fibers • methocarbamol
by preventing the movement of calcium, potassium, and sodium through the • orphenadrine
fibers • tizanidine

Pharmacotherapeutics Pharmacokinetics
general: given so that surgical procedures can be • absorbed in the GIT
performed • widely distributed
local: given so diagnostic, dental, and surgical procedures can be performed; • metabolized in the liver and excreted thru the
also used to treat pain kidneys
• onset: oral is 30 min to 1 hour; duration varies
from 4 to 6 hours
• cyclobenzaprine has the longest duration of 12 to
25 hours
Pharmacodynamics
• do not relax skeletal muscles directly or depress
neuronal conduction, neuromuscular
transmission, or muscle excitability
• depress the CNS
Pharmacotherapeutics
• treat acute, painful musculoskeletal conditions
• usually prescribed along with rest and physical
therapy
Drug Interactions
• interact with other CNS depressants causing
increased sedation, impaired motor function and
respiratory depression
• cyclobenzaprine interacts with MAOIs and can
result in a high body temperature, excitation and
seizures
• methocarbamol can antagonize the cholinergic
effects of the anticholinesterase drugs used to
treat myasthenia gravis
Adverse Reactions
• most frequently seen adverse effects relate to
the associated CNS depression*, GI
disturbances linked to CNS depression of the
parasympathetic reflexes**, hypotension and
arrythmias*, urinary frequency, enuresis, and
feelings of urinary urgency
• chlorzoxazone may discolor the urine, becoming
orange to purplish-red when metabolized and
excreted**
• tizanidine has been associated with liver toxicity
and hypotension in some patients
Peripherally-Acting
• most common is dantrolene sodium*
• major effect is on the muscles**
• high therapeutic doses are toxic to the liver
Pharmacokinetics
• peak is 5 hours after ingestion
• absorbed slowly in the GIT; highly plasma bound
• metabolized in the liver with a half life of 4 to 8
hours and excreted in the urine
• half life for healthy adults is 9 hours; maybe
prolonged for patients with liver dysfunction
Pharmacodynamics
• dantrolene works by acting on the muscle
• interferes with calcium ion release from the sarcoplasmic
reticulum and weakens the force of contraction
Pharmacotherapeutics
• helps manage spasticity especially in patients with cerebral palsy,
MS, SCI, and stroke
• used to treat and prevent malignant hyperthermia
Drug Interactions
• simultaneous use of dantrolene and other CNS depressants, such as
anxiolytics, sedatives, and hypnotics, can increase CNS depression
• if given with estrogen, may lead to increased risk of liver toxicity
Lesson 2 Sedatives, Anxiolytics and Hypnotic Agents
Sedatives and Hypnotics
• sedatives reduce activity or excitement*
• when given in large doses, sedatives are
considered hypnotics**
• 3 main classes of synthetic drugs used as
sedatives and hypnotics are
• benzodiazepines
• barbiturates
• nonbenzodiazepine-nonbarbiturate drugs
Benzodiazepines
• minor tranquilizer; anxiolytic
• therapeutic effects include daytime sedation,
sedation before anesthesia, sleep inducement, relief
on anxiety and tension, skeletal muscle relaxation
and anticonvulsant activity*
• estazolam, flurazepam, lorazepam, quazepam,
temazepam, triazolam
Pharmacokinetics
• absorbed well from the GIT and distributed widely in
the body
• some may be given parenterally
• metabolized in the liver and excreted primarily in the
urine
Pharmacodynamics
• stimulate GABA receptors in the ascending reticular
activating system (RAS) of the brain*
• low dose: decrease anxiety by acting on the limbic
system and other areas of the brain that help
regulate emotional activity; calm and sedate
• high dose: induce sleep**
Pharmacotherapeutics
• Clinical indications include relaxing the patient during
the day of before surgery, treating insomnia,
producing IV anesthesia, treating alcohol withdrawal
symptoms, treating anxiety and seizure disorders
and producing skeletal muscle relaxation
Barbiturates
• major pharmacologic action is to reduce the
overall CNS alertness
• barbiturates that are used primarily as sedatives
and hypnotics include amobarbital, aprobarbital,
butabarbital sodium, mephobarbital, pentobarbital
sodium, phenobarbital, secobarbital sodium
• low dose: depress sensory and motor cortex of
the brain causing drowsiness
• high dose: cause respiratory depression and
death because of their ability to depress all levels
of the CNS
Pharmacokinetics
• absorbed well from the GIT and distributed rapidly
• metabolized in the liver and excreted in the urine
Pharmacodynamics
• depress sensory cortex of the brain, decrease major
activity, alter cerebral function, and produce drowsiness,
sedation and hypnosis
Pharmacotherapeutics
• Clinical indications include daytime sedation*, hypnotic
effects for patients with insomnia, preoperative sedation
and anesthesia, relief of anxiety, anticonvulsant effects
• Prolonged use can lead to drug tolerance as well as
psychological and physical dependence
Nonbenzodiazepines-Nonbarbiturates
• act as hypnotics for short-treatment of simple
insomnia
• no special advantages over other sedatives
• include chloral hydrate, ethchlorvynol and
zolpidem
• Lose their effectiveness by the end of the 2nd
week except zolpidem (35 days)
Pharmacokinetics and Pharmacodynamics
• Absorbed rapidly from the GIT, metabolized in
the liver and excreted in the urine
• MOA is not fully known but thought to produce
depressant effects similar to barbiturates
Pharmacotherapeutics
• typically used for short term treatment of simple
insomnia, sedation before surgery and sedation
before EEG studies
Drug Interactions
• common when given with other CNS
depressants causing additive CNS depression
resulting in drowsiness, respiratory depression,
stupor, coma and death
Antianxiety Drugs
• also known as anxiolytics
• used primarily to treat anxiety disorders
• 3 main types
• Benzodiazepines
• Barbiturates
• buspirone
Buspirone
• buspirone hydrochloride is the first anxiolytic in a
class of drugs known as azaspirodecanedione
derivatives
• fewer side effects than some other common
antianxiety drugs
• advantages
• less sedation
• no increase in CNS depressant effects when
taken with alcohol or sedative-hypnotics
• low abuse potential
Pharmacokinetics
• absorbed rapidly; undergoes extensive first pass
effect
• metabolized in the liver and eliminated in the
urine and feces
Pharmacodynamics
• MOA is unknown
• does not affect the GABAreceptors
• produce various effects in the midbrain and act as
a midbrain modulator, possibly due to its high
affinity for serotonin receptors
Pharmacotherapeutics
• used to treat generalized anxiety states
• ineffective when quick relief from anxiety is
needed because of its slow onset of action
Drug Interactions
• does not interact with alcohol or other CNS
depressants
• when given with MAOIs, hypertensive reaction
may occur
Lesson 3 Antidepressants
Antidepressants
• treat affective disorders*
• include
• Monoamine Oxidase Inhibitors (MAOIs)
• Tricyclic Antidepressants (TCAs)
• Selective Serotonin Reuptake Inhibitors
(SSRIs)
MAO Inhibitors
• 2 classifications based on chemical structure
• hydrazines, which include phenelzine sulfate
• nonhydrazines, comprised of a single drug,
tranylcypromine sulfate
Pharmacokinetics
• Absorbed rapidly and completely from the GIT
• Metabolized in the liver to inactive metabolites
• Excreted mainly by the GIT and to a lesser
degree by the kidneys
Pharmacodynamics
• MOA is unclear
• work by inhibiting monoamine oxidase* making
more norepinephrine and serotonin available to
the receptors and thereby relieving the symptoms
of depression
Pharmacotherapeutics
• management of choice for atypical depression**
• may be used to treat typical depression resistant
to other therapies or when other therapies
are contraindicated
• other uses include* phobic anxieties,
neurodermatitis, hypochondriasis and refractory
narcolepsy
Food and Drug Interactions
• MAOI plus antidiabetics = may enhance
hypoglycemic effects
• MAOI plus meperidine = excitation, hypertension
or hypotension, extremely elevated body
temperature and coma
• severe reaction may occur if taken with tyramine*
rich food such as red wines, aged cheese and
fava beans, and sympathomimetic drugs
Tricyclic Antidepressants
• treat major depression, effective and less
expensive than SSRIs and other drugs
• block the uptake of the neurotransmitter
norepinephrine and serotonin
• include amitriptyline hydrochloride,
amitriptyline pamoate, amoxapine,
clomipramine hydrochloride, desipramine
hydrochloride, doxepin hydrochloride,
imipramine pamoate, nortriptyline
hydrochloride, protriptyline hydrochloride and
trimipramine maleate
Pharmacokinetics
• active pharmacologically, some of the metabolites
are also active
• absorbed completely when taken orally but undergo
first-pass effect
• metabolized extensively in the liver and eventually
excreted as inactive compounds
• fat solubility makes these drugs widely distributed,
excreted slowly and long half-lives
Pharmacodynamics
• increase the amount of norepinephrine, serotonin or
both by preventing their reuptake into the storage
granules in the presynaptic nerves
Pharmacotherapeutics
• used to treat episodes of major depression
• effective in treating depression of insidious onset
accompanied by weigh loss, anorexia or insomnia
• physical symptoms may respond after 1 to 2 weeks
of therapy; psychological after 2 to 4 weeks
Drug Interactions
• increase the catecholamine effects of amphetamines and
sympathomimetics leading to hypertension
• barbiturates increase the metabolism of these drugs
and decrease their blood levels
• concurrent use with MAOIs may cause an extremely elevated
body temperature, excitation and seizures
• increased anticholinergic effects when taken with
anticholinergic drugs*
• reduce the antihypertensive effects of clonidine and
guanethidine
Selective Serotonin
Reuptake Inhibitors (SSRIs)
• formerly known as 2nd generation
antidepressants*
• developed to treat depression with fewer side
effects
• chemically different from TCAs and MAOIs
• include:
• citalopram hydrobromide
• fluoxetine hydrochloride
• fluvoxamine maleate
• paroxetine hydrochloride
• sertraline hydrochloride
Pharmacokinetics
• absorbed almost completely after oral
administration and are highly protein bound
• metabolized in the liver and excreted in the
Urine
Pharmacodynamics
• inhibit the neuronal reuptake of the
neurotransmitter serotonin
Pharmacotherapeutics
• used to treat the same major depressive
episodes as TCAs and have the same
degree of effectiveness
• some are used to treat obsessive-compulsive
disorder (OCD)*
• may also be useful in treating panic
disorders, eating disorders, personality
disorders, impulse control and premenstrual
syndrome
Drug Interactions
• associated with the drug’s ability to
competitively inhibit a liver enzyme that is
responsible for oxidation of numerous drugs
• use of drugs with MAOIs can cause serious
potentially fatal reactions
Lesson 4: Antiparkinsonian Agents
2 goals
• promote the secretion of dopamine
(dopaminergic drugs)
• inhibit the cholinergic effects
(anticholinergic drugs)
Anticholinergic
2 chemical categories according to their
chemical structure
• synthetic tertiary amines: benztropine, biperiden
hydrochloride, biperiden lactate, procyclidine, and
trihexyphenidyl
• antihistamines with anticholinergic properties such
as diphenhydramine and orphenadrine
Pharmacokinetics
• well absorbed from the GIT and cross the BBB to
their action site in the brain
• most are metabolized in the liver and excreted by
the kidneys as metabolites and unchanged drug
• unknown distribution
Pharmacodynamics
• high acetylcholine levels produce an excitatory effect
on the CNS, which can cause parkinsonian tremors
• the drugs inhibit the action of acetylcholine at the
receptor sites in the CNS andANS, thus reducing
tremors
Pharmacotherapeutics
• all forms of parkinsonism
• most common in early stages of the disease when the
symptoms are mild and do not have a major impact
on the patient’s lifestyle
• effectively control sialorrhea and 20% effective in
reducing incidence and severity of akinesia and
rigidity
Drug Interactions
• antipsychotic drugs decrease the effectives of
anticholinergics
• OTC cough and cold preparations increase the
anticholinergic effects
Dopaminergic
• Include drugs that are chemically unrelated
• levodopa, the metabolic precursor to dopamine
• carbidopa-levodopa, a combination drug
composed of carbidopa* and levodopa
• amantadine, an antiviral drug
• bromocriptine, a semisynthetic ergot alkaloid
• pergolide and pramipexole, two dopamine
agonists
• selegiline, a MAOI
Pharmacokinetics
• absorbed from the GIT into the bloodstream and are
delivered to their action site in the brain
• absorption is slowed and reduced when ingested with
food
• levodopa is widely distributed in body tissues
• metabolized extensively in various areas of the body
and eliminated by the liver, the kidneys or both
Pharmacodynamics
• act in the brain to improve motor function in or two
ways – increasing dopamine concentration and/or
enhancing the neurotransmission of dopamine
Pharmacodynamics
• levodopa is inactive until it crosses the BBB and is
converted to dopamine by enzymes in the brain,
increasing dopamine concentration in the basal ganglia
• carbidopa enhances levodopa’s effectiveness
• amantines increase the amount of dopamine in the brain
by increasing dopamine release or by blocking dopamine
reuptake from presynaptic neurons
• bromocriptine and pramipexole stimulate dopamine
receptors in the brain, producing effects that are similar to
dopamine’s
• pergolide directly stimulates post synaptic dopamine
receptors in the CNS
• selegiline can increase dopaminergic activity by inhibiting
MAO activity
Pharmacotherapeutics
• to treat patients with severe parkinsonism or those
who do not respond to anticholinergics alone
• levodopa is the most effective drug used to treat
Parkinson’s disease*
• some (amantadine, pramipexole, bromocriptine)
must be tapered to avoid precipitating parkinsonian
crisis and possible life-threatening complications
Adverse Reactions
• levodopa: nausea and vomiting, orthostatic
hypotension, anorexia, neuroleptic malignant
syndrome*, arrythmias, irritability, confusion
• amantadine: orthostatic hypotension, constipation
• bromocriptine: persistent orthostatic hypotension,
ventricular tachycardia, bradycardia, worsening
angina
• pergolide: confusion, dyskinesia**, hallucinations,
nausea
• pramipexole: orthostatic hypotension, dizziness,
confusion, insomnia
Pharmacokinetics
• phenobarbital is absorbed slowly but well from GIT
• 20-45% bound to serum proteins
• 75% is metabolized by the liver
• 25% is excreted in the urine unchanged
Pharmacodynamics
• inhibit impulse conduction in the ascending RAS,
the cerebral cortex, alter cerebellar function,
depress motor nerve output
• stabilize nerve membranes throughout the CNS directly by
influencing ion channels in the cell membrane
Pharmacotherapeutics
• effective in treating partial, tonic-clonic and febrile seizures

Lesson 5 Antiepileptic Agents Adverse Effects

• most common adverse effects relate to CNS depression and its effects
on body function
Anticonvulsant Drugs
• can produce sedation, hypnosis, and deep coma
• also, antiepileptic drugs
• may be associated with physical dependence and withdrawal syndrome
• usually prescribed for long term management of
chronic epilepsy (recurrent seizures) or short-term
Iminostilbenes
management of acute isolated seizures not caused
• most common example is carbamazepine
by epilepsy, such as after trauma or brain injury
• therapeutic serum range is 5-12 mcg/ml
• five major classes
• effectively treats partial and generalized tonic-clonic
• hydantoins
seizures; mixed seizure types
• barbiturates
• iminostilbenes
Pharmacokinetics
• benzodiazepines
• absorbed slowly and erratically from the GIT
• valproic acid
• distributed rapidly to all tissues
• 75-90% protein bound
Hydantoins
• metabolized in the liver and excreted in the urine
• the first anticonvulsant used to treat seizures
• include phenytoin (10-20 mcg/ml), phenytoin
Pharmacodynamics
sodium, fosphenytoin, mephenytoin
• inhibit the spread of seizure activity or
neuromuscular transmission in general
Pharmacokinetics
• phenytoin is absorbed slowly after oral and IM while
Pharmacotherapeutics
mephenytoin is absorbed rapidly after oral
• carbamazepine is the drug of choice in adults and
adminstration
children for treating generalized tonic-clonic seizures
• phenytoin is distributed rapidly in all tissues and
and simple and complex partial seizures
fosphenytoin is widely distributed
Benzodiazepines
Pharmacodynamics
• drugs that provide anticonvulsant effects include
• stabilize nerve cells to keep them from overexcited
• diazepam (parenteral form)
• phenytoin works in the motor cortex of the brain
• clonazepam (recommended for long term
where it stops the spread of seizure activity
treatment of epilepsy; 20-80 ng/ml)
• clorazepate (adjunct therapy in treating partial
Pharmacotherapeutics
seizures)
• phenytoin is the most commonly prescribed
anticonvulsant drug because of its effectiveness
Pharmacokinetics
and low toxicity
• can be given orally or parenterally
• also acts as an antidysrhythmic by increasing the
• absorbed rapidly and almost completely from the
electrical stimulation threshold in cardiac tissue
GIT
• non-addicting but has teratogenic effects on the
• distributed at different rates
fetus
• 85-90% protein-bound
• it’s one of the drugs of choice to manage
• complex partial seizure (psychomotor or
Pharmacodynamics
temporal lobe seizures)
• act as anticonvulsants, anxiolytics, sedativehypnotics, muscle relaxants
• tonic-clonic seizures
• potentiate the effects of GABA*
• Stabilize nerve membranes throughout the CNS to
Adverse Effects
decrease excitability and hyperexcitability to
• May cause severe liver toxicity, bone marrow
stimulation
suppression, gingival hyperplasia*, potentially
serious dermatological reactions**, bone marrow
Pharmacotherapeutics
suppression
• absence, atonic and myoclonic seizures
Barbiturates
Valproic Acid
• long-acting barbiturate phenobarbital was formerly
• unrelated structurally to other anticonvulsants
one of the most widely used anticonvulsants, now
• used cautiously when giving this drug to very young
less frequent due to the adverse effects
children and clients with liver disorders because
• therapeutic serum range for phenobarbital is 15-40
hepatotoxicity is one of the possible adverse
mcg/ml
reaction
• 2 major drugs: valproate (40-100 mcg/ml) and
Divalproex
Pharmacokinetics
• valproate is converted rapidly to valproic acid in the
stomach
• divalproex is a precursor of valproic acid and
separates into valproic acid in the GIT
• absorbed well, strongly protein-bound
• metabolized in the liver and excreted in the urine
Pharmacodynamics
• unknown MOA but thought to increase the level of
GABA
Pharmacotherapeutics
• prescribed for long term treatment of absence,
myoclonic and tonic-clonic seizures
Lesson 6: Antipsychotic Agents
Antipsychotic Agents
• control psychotic symptoms such as delusion,
hallucinations and though disorders that can occur
with schizophrenia, mania and other psychoses*
Various Names
• antipsychotics: eliminate the signs and symptoms of
psychoses
• major tranquilizer: calm an agitated patient
• neuroleptic: can cause an adverse neurobiological effect that
causes abnormal body movements
Major Groups
• typical antipsychotics: phenothiazines and nonphenothiazines
• atypical antipsychotics: clozapine, olanzapine and risperidone
Typical Antipsychotics
• 3 distinct classes of phenothiazines according to
adverse reactions that they can cause
Aliphatics
• primarily cause sedation and anticholinergic effects
and are moderately potent drugs that include
chlorpromazine hydrochloride and promazine
hydrochloride
• strong sedative effect, decrease BP and may cause
moderate EPS (pseudoparkinsonism)
Piperazines
• primarily cause extrapyramidal reactions and include
acetophenazine maleate, fluphenazine decanoate,
fluphenazine enanthate, fluphenazine hydrochloride,
perphenazine and trifluoperazine hydrochloride
• low sedative effect, little effect on BP and strong
antiemetic effect
Piperidines
• primarily cause sedation, and include mesoridazine
besylate and thioridazine hydrochloride
• strong sedative effect, cause few EPS, low to
moderate effect on BP and have no antiemetic effect
-drug classes of non phenothiazines according to
chemical structure
• butyrophenones: haloperidol and haloperidol
decanoate
• dibenzoxazepines: loxapine succinate
• dihydroindolones: molindone hydrochloride
• diphenylbutylpiperidines: pimozide
• thioxanthenes: chlorprothixene, thiothixene and
thiothixene hydrochloride
Pharmacokinetics
• absorbed erratically; very lipid soluble and highlyprotein bound
• distributed in many tissues and highly concentrated
in the brain
• metabolized in the liver and excreted in the urine and
bile
Pharmacodynamics
• work by blocking postsynaptic dopaminergic
receptors in the brain
• phenothiazines stimulate the extrapyramidal system
Pharmacotherapeutics
• Phenothiazines
• schizophrenia
• calm anxious or agitated patients
• improve patient’s thought process
• alleviate delusions and hallucinations
• Non-phenothiazines
• psychotic disorders
• thiothixene: controls acute agitation
• haloperidol and pimozide: Tourette’s Syndrome
Drug Interactions
• increased CNS depressant effects such as stupor if
phenothiazines are taken with CNS depressants; the
drugs may also reduce the phenothiazine
effectiveness resulting in increased psychotic behavior
or agitation
• taking anticholinergic drugs with phenothiazines
may result in increased anticholinergic effects such
as dry mouth and constipation*
• phenothiazines may reduce the antiparkinsonian effects
of levodopa, lower the threshold for seizures if taken with
anticonvulsants, increase the serum levels of TCAs and
beta blockers
• Nonphenothiazines’** dopamine blocking activity can
inhibit levodopa and may cause disorientation in
patients receiving both medications; haloperidol may
boost the effects of lithium, producing encephalopathy
• lesser side effects; most common is weight gain
• 2 advantages over typical antipsychotics
• effective in treating negative symptoms
• not likely to cause EPS
• include
• clozapine
• olanzapine
• risperidone
Pharmacokinetics
• absorbed after oral administration
• metabolized by the liver and highly protein-bound
• eliminated in the urine with a small portion in feces
Pharmacodynamics
• block the dopamine receptors but not as
effectively as the typical antipsychotics, in addition
to blocking serotonin receptor activity
Pharmacotherapeutics
• schizophrenic patients who are unresponsive to
typical antipsychotics
Pharmacodynamics
• drugs that alter the P-450 enzyme system will alter
the metabolism of the atypical antipsychotics
• counteract the effects of levodopa and other
dopamine agonist
MODULE 7 DRUGS ACTING ON RENAL SYSTEM
Diuretics
• promote the excretion of water and electrolytes
by the kidneys
• 2 main purposes: to lower blood pressure and
to decrease edema* in heart failure and renal or
liver disorder
• major diuretics
• thiazide and thiazide-like
• loop
• potassium-sparing
• osmotic
• carbonic-anhydrase inhibitors
Thiazide & Thiazide-like
• sulfonamide derivatives
• include
• thiazide: bendroflumethiazide,
benzthiazide, chlorothiazide*,
hydrochlorothiazide**, hydroflumethiazide,
methyclothiazide, polythiazide,
trichlormethiazide
• thiazide-like: chlorthalidone, indapamide
Pharmacokinetics
thiazide
• absorbed rapidly but incompletely from the GIT
after oral administration
• cross placenta and secreted in the breastmilk
• differ in how well they are metabolized
• thiazide-like
• absorbed from GIT
• excreted primarily in the urine
Pharmacodynamics
• work by preventing sodium from being reabsorbed in
the kidney
• increase the excretion of chloride, potassium and
bicarbonate which can result in electrolyte imbalance
Pharmacotherapeutics
• long term treatment of hypertension and also used to
treat edema caused by mild to moderate heart failure,
liver disease, kidney disease and corticosteroid and
estrogen therapy
• diabetes insipidus*: paradoxically decrease urine volume,
possibly through sodium depletion and plasma volume
reduction
Side Effects and Adverse Reactions
• cause loss of Na, K and Mg but promote Ca reabsorption
• affect glucose tolerance and hyperglycemia can occur**
• block Ca and uric acid secretion leading to hyperuricemia
and hypercalcemia
• increase serum cholesterol, LDL and triglyceride levels
leading to hyperlipidemia
Drug Interactions
• altered fluid volume, blood pressure and serum
electrolyte levels
• may increase blood glucose levels requiring higher doses
of insulin and oral antidiabetic drugs
• taking corticosteroids, corticotropin and amphotericin
may cause hypokalemia
• risk of digoxin toxicity increases due to potential changes
in potassium levels
• risk of lithium toxicity may increase if these drugs are
combined
Loop Diuretics
• high ceiling diuretics
• act on the thick ascending loop of Henle to inhibit
chloride transport of Na into the circulation
• include bumetanide, ethacrynate sodium,
ethacrynic acid, torsemide and furosemide
Pharmacokinetics
• absorbed well and distributed rapidly
• highly protein bound
• undergo partial or complete metabolism in the
liver except for furosemide, which is excreted
primarily unchanged
• excreted by the kidneys
Pharmacodynamics
• most potent drugs available
• high potential for causing severe adverse reactions
• act primarily on the thick ascending loop of Henle to
increase the secretion of sodium, chloride and water;
may also inhibit the reabsorption of these substances
Pharmacotherapeutics
• edema associated with heart failure
• hypertension: usually with a potassium-sparing
diuretic or a potassium supplement to prevent
hypokalemia
• edema associated with liver disease of nephrotic
Syndrome
Adverse Reactions
• reduced blood volume, orthostatic hypotension,
hyponatremia, hypokalemia, hypocalcemia,
hypomagnesemia, hypochloremia
Drug Interactions
• increased risk of ototoxicity when taken together with
aminoglycosides and cisplatin
• reduce the hypoglycemic effect of oral antidiabetic
drugs, possibly resulting in hyperglycemia
• may increase risk of lithium toxicity
• increased risk of electrolyte imbalances that can
trigger arrhythmias when taken together with digitalis
glycosides
Potassium-Sparing Diuretics
• have weaker diuretic and antihypertensive effects
than other diuretics but have the advantage of
conserving potassium*
• include amiloride, spironolactone and triamterene
Pharmacokinetics
• available orally and absorbed in the GIT
• metabolized in the liver except for amiloride
• excreted primarily in the urine and bile
Pharmacodynamics
• urinary excretion of sodium and water increases as
does the excretion of chloride and calcium ions
• excretion of potassium and hydrogen ion
decreases
• spironolactone* is structurally similar to
aldosterone and acts as aldosterone antagonist
Pharmacotherapeutics
• edema
• diuretic-induced hypokalemia in patients with heart
failure
• cirrhosis
• nephrotic syndrome
• hypertension
• hyperaldosteronism and hirsutism including
hirsutism associated with Stein-Leventhal
Syndrome
• commonly used with other diuretics to potentiate
their action or counteract their K-wasting effects
Adverse Reactions
• few with these drugs
• can lead to hyperkalemia especially when taken
together with potassium supplement or a high
potassium diet
Osmotic Diuretics
• pull water into the renal tubule without sodium loss
• example is mannitol*
• effects are not limited to kidneys because the
injected substance pulls fluid into the vascular
system from extravascular spaces, including the
aqueous humor
• used in acute situations when it is necessary to
decrease IOP before eye surgery or during acute
attacks of glaucoma
• diuretic of choice in cases of increased ICP or acute
renal failure due to shock, drug overdose or trauma
Pharmacokinetics
• mannitol is only available for IV use
• freely filtered at the renal glomerulus, poorly
reabsorbed by the renal tubule and resistant to
metabolism *
• action depends on the concentration of osmotic
activity in the solution
Contraindications and cautions
• mannitol is contraindicated in patients with renal
disease and anuria from severe renal disease,
pulmonary congestion, intracranial bleeding,
dehydration and heart failure
Adverse Effects
• the most common and potentially dangerous
adverse effect is the sudden drop in fluid levels
• nausea, vomiting, hypotension, light headedness,
confusion, and headache can be accompanied by
cardiac decompensation and even shock
• patients receiving this drug should be closely
monitored for fluid and electrolyte imbalance
Carbonic Anhydrase Inhibitors
• mild diuretics
• include acetazolamide and methazolamide
Pharmacokinetics
• rapidly absorbed and widely distributed
• can be orally or IV
• drugs peak in 2-4 hours, 15 minutes if given IV;
duration is 6-12 hours
• excreted in the urine
• have been associated with fetal abnormalities, and
should not be used during pregnancy
Pharmacodynamics
• block the effects of carbonic anhydrase thereby
slowing down the movement of hydrogen ions; as a
result, more sodium and bicarbonate are lost in the
urine*
• used as adjuncts to other diuretics when a more
intense diuresis is needed
• used to treat glaucoma
Adverse Effects
• related to disturbances in acid-base and electrolyte
balances such as metabolic acidosis and
hypokalemia
• others include paresthesia*, confusion, and
drowsiness**
Drug Interactions
• there may be an increased excretion of salicylates
and lithium if they are combined with these drugs.
Lesson 2: Drugs for Fluid & Electrolyte Balance
Introduction
• illness can easily disturb the homeostatic
mechanisms that help maintain fluid and
electrolyte balance
• loss of appetite, medication administration,
vomiting, surgery and diagnostic tests can also
alter the balance
• electrolyte is a compound or element that carries
an electrical charge when dissolved in water
• electrolyte replacement drugs are mineral salts
that increase depleted or deficient electrolyte
levels
Potassium
• major cation in ICF
• adequate amounts must be ingested daily*
• potassium supplement can be accomplished
orally or IV with potassium salts, such as
potassium bicarbonate, potassium chloride,
potassium gluconate, potassium sulfate
• normal amount: 3.5-5.5 mEq/L
• dietary requirement: 40-60 mEq
Pharmacokinetics
• absorbed readily from GIT
• after absorption into the ECF, almost all
potassium passes into the ICF
• normal serum levels of potassium are
maintained by the kidneys, which excrete most
of the excessive potassium intake; the rest is
excreted in the feces and sweat
Pharmacodynamics
• moves quickly into the ICF to restore depleted
potassium levels and re-establish balance
• essential element in determining cell membrane
potential and excitability
• necessary for proper functioning of all nerve and
muscle cells for nerve impulse transmission
• essential for tissue growth and repair and for
maintenance of acid-base balance
• needed for enzyme action used to change
carbohydrates to energy and amino acids to
proteins
Pharmacotherapeutics
• vomiting or diarrhea; excessive urination; some
kidney diseases; cystic fibrosis; burns; excess of
antidiuretic hormone (ADH) or therapy with a
potassium-depleting diuretic; alkalosis;
insufficient potassium intake from starvation;
administration of a glucocorticoid, IV
amphotericin or IV solutions that contain
insufficient potassium; used to decrease the
toxic effects of digoxin
Adverse Reactions
• oral potassium sometimes causes nausea, vomiting,
abdominal pain, and diarrhea
• enteric coated tablets may cause small bowel ulceration,
stenosis, hemorrhage and obstruction
• IV infusion of potassium preparations can cause pain at
the injection site and phlebitis
• if given rapidly, IV administration may cause cardiac arrest
• infusion of potassium in patients with decreased urine
production increases the risk of hyperkalemia
Drug Interactions
• Should be used cautiously in patients receiving
potassium-sparing diuretics or ACE inhibitors to avoid
hyperkalemia
Calcium
• almost all calcium in the body is stored in the
bone, where it can be mobilized if necessary*
• chronic insufficient calcium intake can result in
bone demineralization
• promotes normal nerve and muscle activity and
increases the contraction of the heart’s muscle
• replaced orally or IV with calcium salts, such as
calcium carbonate, calcium chloride, calcium
citrate, calcium gluconate, calcium glubionate,
calcium lactate
• normal amount: 4.5 to 5.5 mEq/L or 8.5 to 10.5
mg/dl
• daily requirement: 1,300 mg (14-18); 1,000 mg
(19-50 yo); 1,200 mg (above 50 yo)
Pharmacokinetics
• absorbed readily from the duodenum and
proximal jejunum
• pH of 5 to 7, parathyroid hormone and vitamin D
all aid calcium absorption
• distributed primarily I the bone
• calcium salts are eliminated primarily in the
feces; the rest is excreted in the urine
Pharmacodynamics
• extracellular ionized calcium plays an essential
role in normal nerve and muscle excitability
• calcium is integral to normal functioning of the
heart, kidneys and lungs and it affects the blood
coagulation* rate as well as cell membrane and
capillary permeability
• calcium is a factor in neurotransmitter and
hormone activity, amino acid metabolism, vitamin
B12 absorption and gastrin secretion
• plays a major role in normal bone and tooth
formation
Pharmacotherapeutics
• helpful in treating magnesium intoxication
• strengthen myocardial tissue after defibrillation
• pregnancy and breast-feeding
• major indication for IV calcium is acute
hypocalcemia: tetany, cardiac arrest, vitamin D
deficiency, parathyroid surgery, and alkalosis
• oral calcium is used to supplement a calciumdeficient diet and prevent
osteoporosis, chronic
hypocalcemia, osteomalacia, rickets and vitamin
D deficiency
Adverse Reactions
• hypercalcemia: early signs include drowsiness,
lethargy, muscle weakness, headache,
constipation, metallic taste in the mouth
• ECG: elevated serum calcium levels may lead to
a shortened QT interval and heart block
• severe hypercalcemia can cause cardiac
arrhythmias, cardiac arrest, and eventually coma
Drug Interactions
• preparations administered with digoxin may
cause arrhythmias
• calcium replacement drugs may reduce the
response to calcium channel blockers
• calcium replacements may inactivate
tetracyclines
• calcium supplements may decrease the
amount of atenolol available to the tissues
resulting in decreased effectiveness of the
drug.
Magnesium
• most abundant cation in ICF after potassium
• essential in transmitting nerve impulses to muscle
and activating enzymes necessary for
carbohydrate and protein metabolism
• stimulates parathyroid hormone secretion thus
regulating ICF calcium levels
• aids in cell metabolism and the movement of
sodium and potassium across cell membranes
• typically replaced in the form of magnesium
sulfate
• normal value: 1.5-2.5 mEq/L
• daily requirement: 19-30 years, 400 mg (men)
and 310 mg (women); 31 years and older, 420 mg
(men) and 320 mg (women)
Pharmacokinetics
• distributed widely throughout the body; IV
magnesium sulfate acts immediately, whereas
after IM administration, it acts within 30 minutes
• not metabolized and is excreted unchanged in the
urine; some are excreted in the breast milk
Pharmacodynamics
• replenishes and prevents magnesium
deficiencies; also prevents seizures by blocking
neuromuscular transmission
Pharmacotherapeutics
• DOC for replacement therapy in magnesium deficiency
• seizure, severe toxemia and acute nephritis in children
Drug Interactions
• may lead to heart block if given together with digoxin
• may increase CNS depressants if given with alcohol,
narcotics, antianxiety drugs, barbiturates,
antidepressants, hypnotics, antipsychotics or general
anesthetics
Adverse Reactions
• life threatening ARs include hypotension, circulatory
collapse, flushing, depressed reflexes, respiratory
paralysis
Sodium
• major cation in ECF
• maintains the osmotic pressure and concentration
of ECF, acid-base balance and water balance
• contributes to nerve conduction and
neuromuscular function
• replacement is necessary for conditions that
deplete it such as excessive GI fluid loss and
excessive perspiration
• normal value: 135-145 mEq/L
• daily dietary requirement: 2 g
Pharmacokinetics Pharmacokinetics
• oral and parenteral preparations are quickly absorbed • cimetidine, nizatidine, and ranitidine are
and distributed widely throughout the body absorbed rapidly and completely from GIT
• not significantly metabolized, primarily eliminated in the • famotidine is not absorbed completely
Urine • food and antacids may reduce absorption
• distributed widely through the body, metabolized
Pharmacodynamics by the liver and excreted in the urine
• replaces deficiencies of the sodium and chloride ions in
the blood plasma Pharmacodynamics
• block histamine from stimulating the acid-secreting
Pharmacotherapeutics parietal cells of the stomach
• water and electrolyte replacement in patients with • blocking gastric acid secretions and promote healing of
hyponatremia from electrolyte loss of severe sodium ulcer by eliminating its cause
chloride depletion
Pharmacotherapeutics
Drug Interactions and Adverse Reactions • treatment of active duodenal ulcer or benign gastric ulcer
• no significant drug interactions except for some reports • treatment of pathologic GI hypersecretory conditions such as
when taken with lithium and tolvaptan Zollinger-Ellison Syndrome
• adverse reactions include pulmonary edema, • reduce gastric acid production and prevent stress ulcers in severely
hypernatremia and potassium loss ill patients and in those with reflux esophagitis or upper GI
bleeding
• treatment of erosive gastroesophageal reflux
• relief of symptoms of heartburn, acid indigestion, and sour stomach
MODULE 8: Drugs Acting on the Gastrointestinal System
Drugs and GI System Drug Interactions
• GIT is basically a hollow, muscular tube that • antacids reduce the absorption of cimetidine,
begins at the mouth and ends at the anus nizatidine, and famotidine
• encompasses the pharynx, stomach, and the • cimetidine may increase the blood levels of oral
small and large intestines anticoagulants, propranolol, benzodiazepines,
• to digest and absorb food and fluids and excrete TCAs, theophylline, procainamide, quinidine,
metabolic wastes lidocaine, phenytoin, calcium channel blockers,
cyclosporine, carbamazepine and narcotic
Lesson 1 Antiulcerant Drugs analgesics by reducing their metabolism in the
Antacids liver and subsequent excretion
• group of inorganic chemicals that neutralize • cimetidine inhibits metabolism of ethyl alcohol in
stomach acid the stomach, resulting in higher blood alcohol
• OTC levels
• used alone or with combination with other drugs
to treat peptic ulcers* Adverse Reactions
• include magnesium hydroxide, aluminum • headache, dizziness, malaise, muscle pain, nausea,
hydroxide, simethicone, magaldrate (aluminummagnesium complex), calcium diarrhea or constipation, rashes, itching, loss of sexual
carbonate, desire and impotence
sodium bicarbonate • famotidine and nizatidine produce few adverse reactions
with headache as the most common followed by
Pharmacokinetics constipation or diarrhea and rash
• neutralize gastric acid*
• distributed throughout the GIT and are eliminated Proton Pump Inhibitors
primarily in the feces • disrupt the chemical binding in the stomach cells
to reduce acid production, lessening irritation and
Pharmacodynamics allowing peptic ulcers to better heal*
• the acid-neutralizing action of antacids reduces • include rabeprazole, pantoprazole, omeprazole,
the total amount in the GIT allowing peptic ulcers lansoprazole, esomeprazole
time to heal
Pharmacokinetics
Pharmacotherapeutics • given orally in enteric-coated formulas to bypass
• used alone or with other drugs to relieve pain and the stomach because they’re highly acid labile
promote healing in PUD • when in small intestine, they are dissolved, and
• relieve symptoms of acid indigestion, heartburn, absorption is rapid
dyspepsia or GERD • highly protein-bound and are extensively
metabolized by the liver to inactive compounds
Drug Interactions then eliminated in the urine
• interfere with the absorption of oral drugs if given at the
same time Pharmacodynamics
• absorption of digoxin, iron salts, isoniazid, quinolones, • block the last step in the secretion of gastric acid
and tetracyclines may be reduced if taken within 2 by combining with hydrogen, potassium and
hours of antacids adenosine triphosphate in the parietal cells of the
stomach
H2 Receptor Antagonists
• H2 blockers Pharmacotherapeutics
• commonly prescribed include cimetidine, • short term treatment of active gastric ulcers,
nizatidine, ranitidine and famotidine active duodenal ulcers, erosive esophagitis,
symptomatic GERD that is not responsive to
other therapies, active peptic ulcers associated
with H. pylori infection in combination with
antibiotics, long term treatment of hypersecretory
states such as Zollinger-Ellison syndrome
Drug Interactions
• interfere with the metabolism of diazepam, phenytoin
and warfarin causing increased half-lives and elevated
plasma concentrations of these drugs
Contraindications
• known allergy to the drug or its components
• caution in pregnant or lactating women
Side Effects and Adverse Reactions
• CNS effects of dizziness and headache are common; GI
effects include abdominal pain, diarrhea, nausea and
vomiting, dry mouth and tongue atrophy; URT symptoms
include cough, stuffy nose, hoarseness, and epistaxis
Other Peptic Ulcer Drugs
Sucralfate
• gastrointestinal protectant
• works locally in the stomach, rapidly reacting with
hydrochloric acid to form a thick, paste-like
substance that adheres to the gastric mucosa and
especially to ulcers
• also inhibits pepsin activity in gastric juices,
preventing further breakdown of proteins in the
stomach, including the protein wall of the stomach
• rapidly absorbed after oral administration,
metabolized in the liver, and excreted in the feces; it
crosses the placenta and may enter breast milk
• should not be given to any person with known allergy to the
drug or any of its components to prevent hypersensitivity
reactions
• should not be given to individuals with renal failure or
undergoing dialysis
• caution in patients who are pregnant or lactating
• adverse effects associated with this drug are primarily related
to its GI effects such as constipation, diarrhea, nausea,
indigestion, gastric discomfort, and dry mouth; others include
dizziness, sleepiness, vertigo, skin rash, and back pain
• if aluminum salts are combined with sucralfate, there is a risk
of high aluminum levels and aluminum toxicity; sucralfate
decreased serum levels of phenytoin, fluoroquinolone or
penicillin
Misoprostol
• synthetic prostaglandin
• inhibits gastric acid secretion and increases
bicarbonate and mucus production in the
stomach thus protecting the stomach lining
• primarily used to prevent NSAID-induced gastric
ulcers in patients who are at risk for
complications from a gastric ulcer
• given orally; rapidly absorbed from the GIT,
metabolized in the liver, and excreted in the
urine; crosses placenta and enters breast milk
• contraindicated to patients with allergy to any part
of the drug
• contraindicated during pregnancy because it is an
abortifacient
• caution should be used during lactation and in patients
with hepatic or renal impairment
• adverse effects associated with this drug are primarily
related to its GI effects – nausea, diarrhea, abdominal
pain, flatulence, vomiting, dyspepsia, and constipation;
Genitourinary effects – which are related to the actions of
prostaglandins on the uterus, include miscarriages,
excessive bleeding, spotting, cramping, hypermenorrhea,
dysmenorrhea, and other menstrual disorders
Lesson 2 Laxatives
Chemical Stimulants
• directly stimulate the nerve plexus in the intestinal
wall, causing increased movement and the
stimulation of local reflexes
• include bisacodyl (Dulcolax), cascara, castor oil,
and senna (Senokot)
Pharmacokinetics
• most of these agents are minimally absorbed and
exert their therapeutic effect directly in the GIT
• castor oil has an onset of action of 2-6 hrs;
6-8 hrs (others)
Pharmacotherapeutics
• castor oil is used when a thorough evacuation of
the intestine is desired
• bisacodyl acts in a similar manner but is somewhat
milder in effect; can also be given in a water
enema to stimulate the activity in lower GIT
• cascara is milder than castor oil and is often used
when effects are needed overnight
• senna is available orally in tablet and syrup form
and as a rectal suppository
Contraindications and Cautions
• allergy to any component of the drug
• acute abdominal disorders (appendicitis, diverticulitis,
and ulcerative colitis)
• use with caution in patients with heart block, coronary artery
disease, or debilitation
• use with caution in pregnancy and lactation
Adverse Effects
• GI effects such as diarrhea, abdominal cramping, and nausea
(most common)
• CNS effects such as dizziness, headache, and weakness
• sweating, palpitations, flushing and fainting
• cathartic dependence
Bulk Stimulants
• also known as mechanical stimulants
• rapid-acting, aggressive laxatives that cause the
fecal matter to increase in bulk
• include magnesium sulfate (Epsom salts),
magnesium citrate (Citrate of Magnesia),
magnesium hydroxide (Milk of Magnesia),
lactulose (Constilac), polycarbophil (FiberCon),
psyllium (Metamucil), polyethylene glycol
(MiraLax), polyethylene glycol electrolyte solution
(GoLYTELY), and sodium picosulfate with
magnesium oxide (Prepopix)
Pharmacokinetics
• taken orally
• directly effective within the GIT and are not generally
absorbed systemically
• rapidly acting, causing effects as they pass through the GIT
Contraindications and Cautions
• allergy to the drug or any of its components
• acute abdominal disorders
• used with caution in heart block, CAD, debilitation, pregnancy
and lactation
• polyethylene and glycol electrolyte solution should be used
with caution in any patient with history of seizures
• use with caution and take bulk laxatives with plenty of water
Pharmacotherapeutics
• lactulose, a saltless osmotic laxative that pulls fluid out of the venous
system
and into the lumen of the small intestine
• magnesium citrate and hydroxide, milder and slower-acting laxatives and
work by saline pull
• magnesium sulfate, exerts a hypertonic pull against the mucosal wall
• polycarbophil, stimulates local activity; milder and less irritating than many
other bulk stimulants
• polyethylene glycol and polyethylene glycol electrolyte solution, hypertonic
fluids containing many electrolytes that pull fluid out of the intestinal wall to
increase the bulk of intestinal contents
• psyllium, gelatin-bulk stimulant; similar to polycarbophil in action and effect
• sodium picosulfate with magnesium oxide provides a combination
stimulant laxative with a bulk laxative
Adverse Effects
• GI effects such as diarrhea, abdominal cramping, and
nausea
• CNS effects including dizziness, headache and
weakness
• sweating, palpitations, flushing, and fainting
Drug Interactions
• the administration of laxatives and other medications
should be separated by at least 30 minutes
• increased risk of neuromuscular blockade when using
nondepolarizing neuromuscular junction blockers with
magnesium salts
Lubricants
• make defecation easier without stimulating the
movement of the GIT
• include docusate (Colace), glycerin (Sani-Supp), and
mineral oil
Pharmacotherapeutics
• docusate has a detergent action on the surface of the
intestinal bolus
• glycerin is hyperosmolar laxative that is used in
suppository form to gently evacuate the rectum without
systemic effects higher in the GIT
• mineral oil is the oldest of these laxatives; not
absorbed and forms a slippery coat on the contents of
the intestinal tract
Pharmacokinetics
• not absorbed systemically and are excreted in the
feces
• docusate and mineral oil are given orally
• glycerin is available as a rectal suppository or as a
liquid for rectal retention
Contraindications and Cautions
• allergy to any component of the drug
• acute abdominal disorders
• used with caution in heart block, CAD, and debilitation
• caution should be used during pregnancy and
lactation
Adverse Effects
• most common are GI effects such as diarrhea,
abdominal cramping, and nausea
• leakage and staining may be a problem when mineral oil
is used, and the stool cannot be retained by external
sphincter
• CNS effects including dizziness, headache, and
weakness are not uncommon
• sweating, palpitations, flushing, and fainting have been
reported after laxative use
Drug Interactions
• frequent use of mineral oil can interfere with the
absorption of the fat-soluble vitamins A,D,E and K
Lesson 3 Gastrointestinal Stimulants
Gastrointestinal Stimulants
• stimulate parasympathetic activity or make the GI
tissues more sensitive to parasympathetic activity
• include dexpanthenol (Ilopan) and metoclopramide
(Reglan)
Pharmacotherapeutics
• increase GI secretions and motility on a general level
throughout the tract
• indicated when more rapid movement of GI contents is
desirable
• dexpanthenol works by increasing acetylcholine levels
and stimulating the parasympathetic system
• metoclopramide works by blocking dopamine receptors
and making GI cells more sensitive to acetylcholine
Pharmacokinetics
• dexpanthenol is given by IM and reaches peak levels
within 4 hours
• metoclopramide is given orally or by IM or IV infusion and has a
peak effect by all routes in 60-90 mins
• metabolized in the liver and excreted in the feces and urine
• metoclopramide crosses the placenta and enters breast milk
• dexpanthenol may cross the placenta and enter breast milk
Contraindications and Cautions
• should not be used in patients with a history of allergy to any of
these drugs or with GI obstruction or perforation
• should be used with caution during pregnancy or lactation
Adverse Effects
• most common effects include nausea, vomiting, diarrhea,
intestinal spasm, and cramping
• others include declining blood pressure and heart rate,
weakness and fatigue
Drug Interactions
• metoclopramide has been associated with decreased
absorption of digoxin from the GIT**
• decreased immunosuppressive effects and increased toxicity of
cyclosporine have occurred when combined with
metoclopramide
• increased sedation can occur if either of these drugs is
combined with alcohol or other CNS sedative drugs
Lesson 4 Antidiarrheals
Antidiarrheals
• block stimulation of the GIT for symptomatic relief from
diarrhea
• include bismuth subsalicylate, crofelemer, loperamide,
opium derivatives
Pharmacotherapeutics
• slow the motility of the GIT through direct action on the lining
of the GIT to inhibit local reflexes (bismuth subsalicylate)
through direct action on the muscles of the GIT to slow activity
(loperamide), or through action on CNS centers that cause GI
spasm and slowing (opium derivatives)
• indicated for the relief of symptoms of acute and chronic
diarrhea, reduction of volume of discharge from ileostomies,
and prevention and treatment of traveler’s diarrhea*
Pharmacokinetics
• bismuth subsalicylate is absorbed from the GIT after oral
administration, metabolized in the liver, and excreted in
the urine; it crosses the placenta*
• loperamide is slowly absorbed after oral administration,
metabolized in the liver, and excreted in the urine and
feces; it may cross the placenta and enter breast milk
• opium derivative, a category C-III controlled substance,
is readily absorbed after oral administration, metabolized
in the liver, and excreted in the urine; crosses the
placenta and enters breastmilk
• Crofelemer is minimally absorbed, and its half-life,
metabolism, and excretion are unknown

Contraindications and Cautions

• should not be given to anyone with known allergy to the
drug or any of its components
• caution should be used in pregnancy and lactation
• care should be taken in individuals with any history of GI
obstruction and acute abdominal conditions or diarrhea due
to poisonings or with hepatic impairment

Adverse Effects
• constipation, distention, abdominal discomfort, nausea,
vomiting, dry mouth, and toxic megacolon
• others include fatigue, weakness, dizziness, and skin rash
• opium derivatives are also associated with light headedness,
sedation, euphoria, hallucinations and respiratory
depression
#continuation of lec.
Informatic Nurses &Informatics Nurse Specialist

American Nursing Informatics Association (ANIA)

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-Has annual educational conferences, provides continuing education forums,
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members also receive a discounted subscription rate for Computers,
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International Medical Informatics Association (IMIA)

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