MODULE 10

Pharmacology II
 Lifespan Considerations
 Pregnant Women
 If possible, drug therapy should be delayed until
after the first trimester, especially when there is
danger of drug-induced developmental defects.
 Potential fetal risks must be compared to
maternal benefits when drug therapy is required.
 Minimum therapeutic dose should be used for as
short a time period as possible.

2
 Lifespan Considerations (cont’d)
 Pregnant Women
 FDA Pregnancy Categories:
 Drugs in categories A and B most likely

carry little or no risk to the fetus.

 Drugs in categories C and D most likely
carry some risk to the fetus.
 Drugsin category X are contraindicated
during pregnancy.

3
Lifespan Considerations (cont’d)
 Pregnant Women
 There are certain situations that require
judicious use of drugs during pregnancy:
 Hypertension
 Epilepsy
 Diabetes
 Infections that could seriously endanger the
mother and fetus

4
Lifespan Considerations (cont’d)
 Breast-feeding Women
 Many drugs cross from the mother’s circulation
into breast milk and subsequently to the infant,
although in small amounts because this is not
the primary excretion route.
 Again, the risk to benefit ratio must be
evaluated.

5
Lifespan Considerations (cont’d)
 Children
 Parent is important source of:
 Information about the child

 Source of comfort for the child

 Partner with the health care team during

drug therapy.
 Should not be used to refer to a patient under
1 year of age.

6
Lifespan Considerations (cont’d)
 Children
 Differences in Physiology and
Pharmacokinetics
 Immaturity of organs most responsible

 Anatomic structures and physiologic

systems and functions are still in the

process of developing

7
Lifespan Considerations (cont’d)
 Children
 Pharmacodynamics (Drug Actions)
 Some drugs may be more toxic in children and
some less.
 More toxic – Phenobarbital, morphine, ASA

 Same – Atropine, codeine, digoxin

 Contraindicated – tetracycline (discolor teeth),

corticosteroids (may suppress growth)
Fluoroquinolone antibiotics (may damage
cartilage leading to gait deformities)
 Some tissues may be more sensitive – smaller
doses
8
Lifespan Considerations (cont’d)
 Children - Kid Facts
 Safe, appropriate drug therapy must reflect the
differences between adults and children.
 The child’s stage of growth and development
must be considered when assessing core
patient variables and the interaction of core
drug knowledge and core patient variables.
 Pediatric drug dosages must be accurate to
reduce risk of adverse effects and prevent over
dosage.

9
Lifespan Considerations (cont’d)
 Children - Drug Administration
 Choice of appropriate route and/or site of drug
administration will vary by the child’s age and
size and the drug.
 Special techniques may be needed to minimize
traumatic effects to the child:
 EMLA cream can be used to numb an area
prior to an injection.
 A popsicle or ice chips can be used to numb
taste buds before unpleasant-tasting oral
drugs.
 Do not mix drug therapy into infant formula.

10
Lifespan Considerations (cont’d)
 Children – Nursing Responsiblities
 Education about medications should be
provided for the patient, at an appropriate
developmental level, and to the family.
 Implement the “6 Rights.”

 It may often be necessary for 2 nurses to

check the medication(s). Check agency
policy.

11
Lifespan Considerations (cont’d)
 Older adults/Geriatric Considerations
 Share common age-related changes and risk
factors that alter drug administration, dosage
and expected response to drug therapy.
 All pharmacokinetic processes are altered,
placing older adults at higher risk for
adverse drug effects.

12
Lifespan Considerations (cont’d)
 Geriatric Considerations Pharmacokinetics:
 Alterations in absorption are more likely caused
by disease processes.
 Distribution is altered because of:
 Decreased body mass
 Reduced levels of plasma albumin
 Less effective blood-brain barrier
 Hepatic metabolism is slowed.
 Renal efficiency is decreased:
 Serum creatinine levels will remain normal even
though kidney function is impaired.
13
Lifespan Considerations (cont’d)
 Geriatric Considerations-
Pharmacodynamic Changes
 Receptor site changes.
 Blood-brain barrier allows more drug to
enter the brain.
 Normal aging-related decline in organ or
system function occurs.

14
Lifespan Considerations (cont’d)
Geriatric Considerations
o Polypharmacy
 May see multiple MDs for various illnesses and
all may prescribe meds.
 Consume approx 32% of all Rx drugs and 40%
over the counter (OTC) drugs
 Most common Prescriptions –
antihypertensives, insulin, beta blockers,
digitalis, diuretics, potassium (K) supplements
 Most common OTC’s – analgesics, laxatives,
nonsteroidal anti-inflammatory drugs (NSAIDS)
15
Lifespan Considerations (cont’d)

Geriatric Considerations
 Nonadherence – Lack of knowledge or incomplete
knowledge leads to misunderstanding about
medication regime.
 Lifestyle – Choices may have to be made between
food, rent and purchase of medications.

16
Lifespan Considerations (cont’d)
 Geriatric Considerations:
 Simplify the therapeutic regimen.
 Give memory aids (if necessary).

 Give written instructions.

 Determine financial access to drug therapies.

 Assess cultural barriers.

 Titrate the dose upward slowly to minimize

adverse effects.

17
 Cultural Considerations in
Drug Therapy
 The Law of Cultural Diversity
 Each patient needs to be considered an
individual, regardless of cultural, ethnic or
religious beliefs.
 Although members of a culture share certain
beliefs and practices, individual variation will
still occur. Many cultural groups in the U. S.
have beliefs that reflect both their original
ethnic culture and the dominant culture of the
United States.

18
 Ethnic Considerations in
Drug Therapy
 Drug polymorphism
 Critical in understanding a patient’s response to drug
therapy
 May explain many adverse and idiosyncratic reactions
 Refers to how individuals metabolize differently
 Looks at genetics that often have a common basis in
ethnic background
 Opens up a new field of study in pharmacology that
has been lacking for years due to societal factors
 Examples: Why does the African-American respond
differently to antihypertensives, the Chinese patient
require lower doses of benzodiazepines, the Caucasian
respond differently to some pain medications?
19
 Ethics and
Drug Therapy

Nurse’s responsibility is to always be a patient

advocate and remain nonjudgmental.
 ANA Code of Ethics
 Canadian Nurses Association Code of Ethics
 Various Nurse Practice Acts
 All share the framework for the professional practice of nursing.
 All believe that, professionally, the nurse provides safe nursing
care to patients regardless of the group, community, ethnicity or
culture.
 Nursing does not impose values or standards on the patient.
 Nurses assist the patient and family in facing decisions
regarding health care.
20
Botanical Dietary Supplements
 For a complete list of botanical
dietary supplements fact sheets,
(National Institutes of Health), see :
http://www.ods.od.nih.gov/Health_
Information/Botanical_Supplements
.aspx

21
 The 5th Vital Sign
Pain
Opioid & Non-Opioid Analgesics
Aspirin
NSAIDs
COX-2 inhibitor
Acetaminophen
Narcotics
 Analgesics
Definition of an analgesic:
 “Medications that relieve pain
without causing loss of
consciousness”
 Pain is a subjective experience. The nurse must
believe the patient. PET scans now can
visualize brain’s responses to many kinds of
pain.

23
 Proposed Pain Pathway
Nociceptors (free nerve endings)

Afferent stimulation of sensory “A” or “C”fibers

Release of peptide substance P from unmylinated

“C” fibers in dorsal horn

Dorsal horn spinal cord – the location of the “gate”

3 major brain pathways:

Spinothalamic, spinoreticular, spinomesencephalic
(Multiple neurotransmitters released) 24
 Pathophysiological
Many theories of pain transmission
are not completely understood.
 Nociceptivepain
 Neuropathic pain

 Psychogenic pain

The type of pain determines the analgesic.

Neuropathic pain is often treated with anticonvulsants,

tricyclic antidepressants added onto narcotics 25
 Pain Transmission
These techniques also allow some non-
pharmacological relief from pain:
 Massage
 Deep pressure
 Distraction

 Relaxation

 Vibration

Can be used as independent nursing intervention after

assessment

The above activate the large “A” fibers. 26

 Factors Influencing Pain
Perception

 Type of pain
 Acute vs. chronic
 Visceral vs. cutaneous
 Nociceptive, neuropathic, psychogenic
 Intensity of pain & type of injury
 Inflammatory process

 Degree of Anxiety

27
 Factors Influencing Pain
Perception
 Sensory input
 Social support

 Fatigue

 Age, sex & culture

 Memory & information processing

 Level of consciousness

 Type, amount, route of analgesic

28
Drugs Influencing Pain Perception
Narcotics (opioids) modify pain perception
via Central Nervous System (CNS) & dorsal
horn via binding to Mu, kappa & delta opioid
receptors & inhibiting substance “P” and
glutamate (an excitorary neurotransmitter).
Alter perception of pain via opiate receptors,
and alter psychological responses via brain.

Other mechanisms to alter pain involve effects

on the Autonomic Nervous System (ANS),
skeletal muscle response & diagnosis.
29
Drugs Influencing Pain Perception

 Nonopiate analgesics (salicylates,

NSAIDS, etc.)
 Control pain impulses in the periphery

 Often involving the Arachidonic acid

pathway responsible for inflammation
and an immune response

30
 Some Pain Mysteries

 Phantom pain
 Referred pain
 Pain experienced after cordectomy
 Placebo response

31
 Prostaglandins
 Associated with inflammation
 Involved in the temperature set point
of the hypothalamus
 Sensitize pain receptors to mechanical
and chemical stimulation
 Found in many cells and body
processes

32
 Leukotrines

 Arachidonic acid metabolites

 Mediators in inflammation
 Synthesized when tissue injury occurs
 May be involved in rheumatoid arthritis,
asthma and system wide anaphylaxis
 Bronchoconstrictor and vasodilator

33
 Synthesis of Prostaglandins

Arachidonic acid

enzymes
Lipoxygenase Cyclooxygenase

Leukotrines Prostaglandins

34
 TWO Enzyme FORMS

CYCLOOXYGENASE-1 & CYLOOXYGENASE- 2

COX-1 COX-2
Prostaglandins
Protects stomach lining
Inflammation Pain
35
Peripheral control of pain

Release of prostaglandin
inflammation & pain
Prostaglandins mediate pain and swelling by
triggering vasodilatation. Prostaglandins are
synthesized by the enzyme cyclooxygenase which
breaks down arachidonic acid to synthesize
prostaglandin. This is the basic method of action
of aspirin and NSAIDs.

36
Inhibition of Cox-1 & Cox-2
 Inhibition of both Cox-1 & Cox-2 will be
effective as an:
 ANALGESIC
 ANTIPYRETIC
 ANTI-INFLAMMATORY AGENT
 AGENT TO DECREASE PLATLET
AGGREGATION

 Also associated with stomach damage due

to COX-1 inhibition
37
 Aspirin
 Inhibits both Cox-1 and Cox-2
 Is used as a analgesic
 Is used as a anti-inflammatory agent
 Is used as a antipyretic
 But can cause stomach damage
 Is used to prevent coronary heart disease
(CHD) via platelet aggregation
 In what other cases should aspirin NOT be
used?
38
 Aspirin adverse effects &
interactions
 Tinnitus – sign of toxicity
 Dyspepsia
 Highly protein bound so it displaces other
medications: oral anticoagulants, oral hypoglycemics,
some anticonvulsives.
 G.I. Bleeding increased with glucocorticoids, alcohol
 High doses may cause excessive bruising
 Highly lethal if taken in overdose - No known
antidote
 Caution with asthmatic patients (may have aspirin
allergy also)

39
Hold giving Aspirin

40
 Children under 15 with
viral infection

Reye’s syndrome is associated with aspirin use.

41
 NSAIDS
Non-Steroidal Anti-Inflammatory Drug

 First line treatment for inflammation

 Both COX-1 & COX-2 inhibitors
 Mild to moderate pain of various types
 Good for dysmenorrhea
 Antipyretic
 Reversibly inhibit platelet aggregation (less than
aspirin because aspirin has irreversible
inhibition)
 INHIBIT THE PRODUCTION OF PROSTAGLANDINS
THAT MEDIATE PAIN AND INFLAMMATION

42
 Side effects & Interactions of
NSAIDs

 G.I. Bleeding, dyspepsia

 Liver toxicity or renal damage with large
doses, prolonged use
 Highly bound to plasma protein so
displace other medications, leading to
exacerbation of their side effects
These adverse effects can occur with oral or
parenteral routes and even if enteric coated.
43
Don’t give aspirin or NSAIDs

Patients with ulcers

Patients going to surgery
Patients with an allergy to aspirin
Alcoholic patients
When patient is nauseated or vomiting
Patients on glucocorticoids (without M.D. order)
Patients taking ACEIs (Angiotensin Converting
Enzyme Inhibitors)
Caution with NSAIDs in patients with CHF
44
 COX-2 INHIBITOR

 Celecoxib (Celebrex) Approved for

osteoarthritis and rheumatoid arthritis
 Acute pain & dysmenorrhea

 Do not give if sulfa allergy

Only COX-2 inhibitor currently available

Has anti-inflammatory properties

45
Acetaminophen (Tylenol)
 Is a very weak inhibitor of both Cox-1 and
Cox-2
 Is used as an antipyretic
 Is used as an analgesic
 Can not be used as an anti-inflammatory agent
 Does not stop platelet aggregation
 May work by inhibiting prostaglandin
synthesis in the CNS

46
 Acetaminophen

 Is the drug of choice for mild to moderate pain

 Is often combined with opioids to treat moderate
to severe pain
 Will cause liver failure in LARGE doses or
prolonged use (2.4 to 4 grams/day)
 Liver failure with alcohol due to metabolic
pathways
 Ceiling effect
 Overdose is difficult to treat - use acetylcysteine
47
 Acetaminophen

 Young children, older adults, daily drinkers

of 3 or more alcoholic beverages and those
with kidney or liver disease are at risk for
accidental acetaminophen poisoning
 Acetaminophen found in many
pharmaceuticals
 Vicodin ES (5 tabs Q. D. = 4 gm)
 Tylenol extra-strength (8 tabs = 4 gm)
 What other OTC medications might contain
acetaminophen?
48
 Neuropathic Pain
 Difficult to treat
 Use of opioids does not completely control pain
 Usually add on another medication from a different
class (co-analgesic agents)
 immipramine (Tofranil) Tricyclic antidepressant -TCA
 gabapentin (Neurontin) Anticonvulsant
 Duloxetine (Cymbalta) newest SNRI (serotonin
norephinephrine reuptake inhibitor) - also used for
depression
 Effexor is another medication in this class
 New pregabalin (Lyrica) anticonvulsant - alpha2 - delta
ligand
 + other medication classes

49
 Natural, synthetic and semisynthetic

ALL COMPARED TO MORPHINE

50
 Opiates

Narcotics: Very strong pain relievers

Opiates:
 Pain relievers that contain opium, derived
from opium, or are chemically related to
opium

51
 Pain Transmission

o Body has endogenous neurotransmitters

o Endogenous neurotransmitters are:
enkephalins & endorphins (morphine-like
peptides) produced by body to fight pain
o Opiates bind to these natural endogenous
opioid receptors
o Inhibit substance P in dorsal horn of spinal
cord
52
Chemical Classification of Opioids

CHEMICAL CATEGORY & examples

Natural: codeine, morphine
Semi-synthetic: hydrocodone (Vicodin)
(Percodan) oxycodone + salicylate
Synthetic: meperdine (Demerol) can be
neurotoxic and cause
confusion/seizure - NEVER
give to patients with
Parkinson’s Disease
butalbital (Fiorinal) 53
 Opiates

 Three classifications based on their

actions:
agonist
agonist-antagonist
partial agonist

54
 CNS Opiate effects/uses

 Analgesia
 Cough suppression
 Euphoria
 Reduces fear/anxiety
 Raises pain threshold (decreased awareness)
 Sleep induction
 Respiratory depression
 Pupil constriction (miosis)
 Nausea and vomiting
55
 Peripheral Nervous System
OPIATE Effects

 Constipation

 Urinaryretention
 Diaphoresis & flushing

 Hypotension due to vasodilatation

56
 Narcotic analgesic routes
 PCA example Morphine (acute pain)
 Transdermal example Duragesic patch (fentanyl)
(chronic pain)
 Epidural example fentanyl or morphine
 Oral example MS Contin (morphine)(chronic pain)
 I.M injections example meperidine (acute pain)
(Demerol). Do not give for more than a day –
neurotoxic, lowers seizure threshold, not first line
agent. Metabolite normeperidine neurotoxic and
may cause psychosis in the elderly patient.

57
 Gold Standard is Morphine
No ceiling effect
ADVANTAGES DISADVANTAGES
 Decreased awareness  Hypotension

 Decreased anxiety  Constipation

 Increased sleep  Nausea
 Decreased pain  Respiratory depression
perception  Itching

Secondary effects of cough suppression and

constipation are used therapeutically
58
 Oral Morphine examples
 Oxycontin (oxycodone)
 MS Contin (morphine)
 Kadian (morphine)
 Oramorph SR (morphine)
 Avinza (morphine)
 New Q day dosing (Do not crush, chew or
dissolve the caps or could deliver fatal dose)
 If can not swallow, O.K. to open & sprinkle the
beads on applesauce

59
 Mixed agonist-antagonists
 Pentazocine (Talwin)
 Buprenorphine (Bupreneax)
 Butorphanol (Stadol)
 Ultram (Tramadol) - mechanism of action not
clearly understood, weak bond to opioid receptors
& inhibits reuptake of norepinephrine (NE) &
serotonin (5-HT) may cause chemical dependency
 These medications are rarely used

DO NOT GIVE THESE MEDICATIONS TO PATIENTS WHO

ARE DEPENDENT ON NARCOTICS.

60
 Opiate Antagonists/blockers

 Naloxone (narcan) opiate antagonist

[competitive]

Naltrexone (ReVia) now used to help

alcoholics stay abstinent

61
 Opiates

 Opioid Tolerance:
 a common physiologic result of chronic
opioid treatment

 means larger doses of opioids are required

to maintain the same level of analgesia

62
 Opiates

Physical Dependence
 The physiologic adaptation of the body to
the presence of an opioid

 Opioid tolerance and physical dependence

are expected with long-term opioid
treatment and should not be confused with
psychological dependence [addiction].

63
 Opiates

Psychological Dependence
[addiction]

Apattern of compulsive drug use characterized by

a continued craving for an opioid and the need to
use the opioid for effects other than pain relief

64
 Opiates

 Misunderstanding these terms

leads to ineffective pain
management and contributes to
the problem of under treatment.

65
 Opiates

Physical dependence on opioids is

known when the opioid is abruptly
discontinued or when a opioid
antagonist is administered.
 narcotic withdrawal
 opioid abstinence syndrome

66
 Opiates

 Narcotic withdrawal
 Opioid abstinence syndrome

Manifested as: (flu-like symptoms)

Anxiety, irritability, chills and hot flashes, joint
pain, lacrimation, rhinorrhea, diaphoresis,
nausea, vomiting, abdominal cramps and
diarrhea

67
Drugs Affecting the Autonomic
Nervous System

68
Photo Source: National Institutes of
Health, Public Domain,
http://catalog.niddk.nih.gov/ImageL
ibrary/searchresults.cfm
69
 Sympathetic NS

FIGHT & FLIGHT

70
 Parasympathetic N.S.

BREED & FEED

71
 Adrenergic Drugs
 Mechanism of action
 Mimic Sympathetic Nervous System (N.S.)
 Have sympathomimetic properties
 Have sympatholytic action also since they oppose
the parasympathic N.S.
 Catecholimines are neurotransmitters involved in
adrenergic system
 DA (dopamine) NE (norepinephrine) E (epinephrine)
 Energizing neurotransmitters

 Direct-acting, indirect acting and mixed adrenergics

72
 Adrenergic Drugs (cont’d)
 Indications
 Bronchodilation (albuterol)
 Cardiac stimulation, alpha1, beta 1, beta 2,
increase blood pressure (dopamine, isoproterenol)
 Mental alertness & wakefulness (monafnil)
 Appetite suppression (adipex)
 Decongestion (pseudoephedrine)
 Open angle glaucoma (dipivefrin) produces
mydriasis = pupil dilation
 ADHD (methylphenidate)
 Adverse effects
 Tachycardia, hypertension, anxiety, insomnia,
psychological dependency
73
 Alpha -Adrenergic Blocking
Drugs
 Drug examples: ergotamine tartrate (Egostat),
Phenoxybenzamine, phentolamine (Regitine)
 Indications: Raynaud’s disase, hypertension
secondary to pheochromocytoma, extravasation
of vasopressors, vascular headaches
 Adverse effects: nasal congestion, orthostatic
hypotension, tachycardia, dizziness,
(Gastrointestinal) GI irritation, and miosis.
Ergotamine may cause chronic poisoning.

74
 Beta-Adrenergic Blocking
Drugs
 Drug examples: selective for beta 1 receptors - atenolol,
metoprolol
Non-selective for beta 1 & 2 receptors - propranolol
(contraindicated in pt. with COPD, asthma, depression)
 Indications: treat hypertension, angina,
tachyarrhythmias, CHF, Post MI because they are cardio-
cardio-protective
 Contraindications: bradyarrhythmias, bronchospasm,
heart blocks
 Adverse effects: arrhythmias, bradycardia,
bronchospasm, nausea, vomiting, diarrhea, increased
sensitivity to cold, rebound HTN if stopped abruptly

75
 Cholinergic Drugs
 cholinergics
 cholinergic
agonists
 parasympathomimetics
 Sympatholytics

 All are terms that refer to drugs that stimulate the

Parasympathic Nervous System
 MIMIC ACETYLCHOLINE
 Cholinergic drugs

76
 Cholinergic Drugs
 Cholinergic receptors [two types]
 Based on location & their action

Nicotinic {N}
&
Muscarinic {M}

77
 Drug & Side Effects of
Cholinergics
Salivation
Lacrimation
Urinary incontinence
Diarrhea
Gastrointestinal cramps
Emesis
(Also bronchospasm, decreased intra ocular pressure
(IOP), decreased heart rate, increased bronchial
secretions, miotic, sweating)

78
 Cholinergic Drugs
 Indications
 Direct- acting
 Cholinergic agonists – used to treat open angle glaucoma and dry
eyes and to stimulate bladder
 Indirect-acting
 Cholinesterase inhibitors (reversible) – for Alzheimer’s & to treat
myasthenia gravis (MG) and open angle glaucoma not responsive
to other agents – prevents postoperative paralytic ileus
 Drug examples – bethanechol, pilocarpine
 Bethanechol – treat nonobstructive urine retention, neurogenic
bladder, adynamic ileus
 Pilocarpine – treat glaucoma
 Contraindications
 Possible urinary or GI obstruction and pregnancy
79
 Cholinergic-blocking drugs

 Class of drugs that block or inhibit the

actions of Acetylcholine in the
Parasympathetic Nervous System
 anticholinergics
 parasympatholytics

 antimuscarinic agents

80
 Cholinergic-blocking drugs
(also called anti-cholinergic drugs)

 Inhibit nicotinic {N} or muscarinic {M} receptors

 Anticholinergic effects are the result of
muscarinic blockage, primarily on the post
synaptic receptor of the Parasympathetic
Nervous System.
 There are medications that are designed for their
anticholinergic effect.
 Many medications have anticholinergic side
effects that are NOT wanted.

81
Cholinergic-blocking drugs
 Atropine
 Preop for secretion control, therapeutic
anticholinergic effect, Bradycardia,
anticholinesterase effect for insecticide poisioning
CNS excitation
 Dicyclomine (Bentyl)
 Irritable bowel syndrome (IBS)
 Propantheline bromide (Pro-Banthine)
 Adjunct in Treatment of peptic ulcer, IBS,
pancreatitis

82
Cholinergic-blocking drugs
 Glycopyrrolate (Robinul)
 Control of secretions intraoperative, preop control
of secretions, preop for electro convulsive therapy
(ECT)
 Scopolamine (Transderm-Scop)
 Prevents motion sickness

 Orphendrine (Norflex)
 A central acting anticholinergic muscle relaxant

83
 Therapeutic effects of
Anticholinergics
 Tolterodine (Detrol) & Trospium
Chloride (Sanctura) new
 Overactive bladder
 Benztropine (Cogentin)
 Parkinson’s DZ and EPS (neurological side
effects) from antipsychotics
 Ipratropium Bromide (Atrovent)
 Inhaled drug used to treat COPD, asthma,
little systemic effect because inhaled
84
 Drug Interactions
ADDITIVE EFFECTS WITH: antihistamines,
anticholinergics, phenothiazines,tricyclic
antidepressants, MAOI’s (monoamine oxidase
inhibitor)
Antihistamines have anticholinergic effects

This could cause confusion & or psychosis in the

ELDERLY PATIENT.

Contraindicated in: glaucoma, benign

prostatic hypertrophy (BPH), Cardiac disease and
obstructive bowl & asthma unless inhaled

85
 Secondary effects/Side
effects
(anticholinergic)
 Xerotomia (dry mouth)
 Blurred vision
 Urinary retention
 Decreased perspiration
 Constipation
 Tachycardia
 These are common in many of the psychoactive
drugs
86
 Neuromuscular Blocking
Agents
Prevent nerve transmission in certain muscles,
leading to paralysis of the muscle at neuromuscular
junction by binding to Ach receptor
 Indications – Maintains controlled ventilation
during mechanical ventilation or during
endotracheal intubation
 Contraindications – Drug allergy, previous
history of malignant hypertension, penetrating
eye injuries and narrow-angle glaucoma
 Side/Adverse Effects – Hypokalemia,
dysrhythmias, fasciculations, muscle pain,
increased intraocular and intracranial pressure
and apnea
87
 CNS Depressants
Hypnotics and Sedatives
 Classified into barbiturates,
benzodiazepines and miscellaneous agents
 Act primarily on the brainstem; sedative
and hypnotic effects are dose related.

88
 Barbiturates
 Habit forming and have narrow therapeutic index
 Contraindications –pregnancy, significant
respiratory difficulties and severe liver disease
 Side Effects – Drowsiness, lethargy, dizziness,
hangover, and paradoxical restlessness or excitement
 Adverse Effects – Vasodilatation, hypotension blood
dyscrasias, hypersensitivity reactions
 Interactions – synergistic with other Central Nervous
System (CNS) depressants
 Can be lethal in overdose
 Can have lethal consequences of uncontrolled
withdrawal
89
 Barbiturates Uses
 Short-term treatment of insomnia (rare)
 Sedation in lower doses
 Ultra-short acting for anesthesia induction
 Pre-op medication
 Epilepsy, mainly status, but the long-acting
Phenobarbital can be used as anticonvulsant -
at small doses does not produce sedation, but
seizure activity
 Not used as often today because of newer
agents for sleep, seizure and anxiety

90
Action and General Characteristics
of Benzodiazepines
 Specific for cerebral cortex and limbic system
 Also called anxiolytics
 Increase action of GABA + other inhibitory
neurotransmitters
 Highly lipid soluble to facilitate crossing into
CNS
 Highly bound to plasma protein
 Metabolized by the liver, some with long
duration of action due to active metabolites

91
 Benzodiazepine Uses
 Anxiolytics – examples: alprazolam (Xanax)
 Anticonvulsants – examples: clonazepam
(Klonopin) and diazepam (Valium)
 Anesthesia induction – examples: midazolam
(Versed), diazepam (Valium)
 Muscle Relaxant – example: diazepam (Valium)
 Withdrawal from alcohol – example:
chlordiazepoxide (Librium), diazepam (Valium)
 Hypnotics – examples: flurazepam (Dalmane), and
temazepam (Restoril) do not depress REM sleep;
but prevent deep sleep (not natural)

92
 Secondary/side effects of
Benzodiazipines
 Daytime sedation
 Ataxia
 Dizziness
 Anterograde amnesia
 Idiosyncratic paradoxical excitement
 SELDOM FATAL IF TAKEN ALONE
 Can be dangerous for the elderly because of
fall potential

93
 Centrally Acting Muscle
Relaxants
 Primarily used for the relief of painful
musculoskeletal conditions–muscle spasms
and spasticity.
 Side Effects – Euphoria, lightheadedness,
dizziness, drowsiness, fatigue and muscle
weakness - usually short-lived
 Adverse Effects – GI upset, headache, slurred
speech, constipation, sexual difficulties in
men, hypotension, tachycardia and weight
gain
94
 Anticonvulsant Medication
Causes of Seizure
 Congenital abnormalities
 Metabolic disorders – hypocalcemia
 Trauma – accidents
 Tumors – brain plus status post craniotomy
 Vascular diseases – stroke
 Degenerative disorders- Alzheimer’s
 Infectious diseases – meningitis, AIDS
 Fever & toxins
 Medications – example = antipsychotics
 Alcohol withdrawal + hypomagnesemia 95
 Types of Seizure
according to International League Against Epilepsy

Partial Seizures:
focal area of brain initiates seizure
Simple partial:
focal symptoms, aura, conscious
Complex partial:
simple then impairment in consciousness
Generalized partial:
spread to both hemispheres

96
 Types of Seizure
 Generalized Seizures: both hemispheres
usually effected, unconscious
 Absence seizures: impairment of
consciousness, autonomic components,
usually in children/adolescence
 Tonic-clonic: (grand mal) tonic is muscle
stiffing, clonic is jerking
 Monoclonic: single or multiple jerks

97
 Status Epilepticus
 Single seizure lasting for 20 minutes or
longer
 Or recurrent generalized seizures without
regaining of consciousness in between each
seizure episode
 Considered a medical emergency

98
 Possible Action of
Anticonvulsants
 Pharmacologically distinct action for each
group of anticonvulsants is PROPOSED
 Many mediate actions by limiting discharge
from a focal point – surrounding it
 Others elevate seizure threshold through
neurotransmitters or ions

99
 Possible General Mode of Action

Increase concentration
of GABA by
Blocking reuptake into glia & nerve endings
Inhibiting enzymes that catabolize GABA
Facilitating GABA & other inhibitory
receptors

100
 Mode of Action other than
potentiation of GABA
Suppression of calcium influx
Inhibition of voltage-sensitive sodium channels
Binding to the amino acid glycine
(neurotransmitter & inhibitory A.A.) at receptor
site
Decreasing metabolism of glutamate

EXACT MODE OF ACTION NOT KNOWN

Agent chosen depends on type of seizure, age, sex,
pharmacologic properties, side effects and cost

101
 Anticonvulsants
FIRST LINE AGENTS - USED AS
MONOTHERAPY for Tonic Clonic
Seizures
 Phenytoin ( Dilantin)
 Carbamazepine (Tegretol)
 Valproic acid (Depakene or Depakote)
 Primidone (Mysoline)
 Phenobarbital

102
 Anticonvulsants
 FIRST LINE AGENTS USED AS
MONOTHERAPY for Partial Seizure
 Carbamazepine (Tegretol)
 Valproic Acid (Depakene or Depakote)
 Lamotrigine (Lamictal)
 Topiramate (Topamax)*
 Gabapentin (Neurontin)*
* Not FDA approved for monotherapy, but studies support

103
 Anti-convulsant
Drugs(Antiepilieptics)
 Indications: Prevention and control of seizures
 Main adverse effects of most anticonvulsants are mental
confusion and drowsiness
 Interactions of many older meds:
 Potentiate CNS depressants and alcohol
 Concurrent use with tricyclic antidepressants or phenothaizines
lowers the seizure threshold and decreases the effectiveness of
anticonvulsants
 Many drugs alter hepatic metabolism of anticonvulsants leading
to decreased serum levels and loss of seizure control and toxicity
 Phenytoin’s cytochrome P-450 enymatic reaction inhibits
atazanavir’s action (depakote becomes the drug of choice in this
example).
104
 Anti-convulsant Drugs
 Hydantoins
 Drug examples: Mephenytoin, phenytoin
(Dilantin)
 Indications: treat tonic-clonic (grand mal) seizures
and complex partial seizures, arrhythmias, and
painful condition such as trigeminal neuralgia
 Adverse effects: (long term) gingival hyperplasia,
liver function abnormalities, blood dyscrasias,
(toxicity) as evidenced by diplopia, nystagmus,
ataxia, and drowsiness
 Caution driving or operating equipment because of
mental confusion

105
 Anti-convulsant Drugs
 Tell patient to use alternate birth control
if on the pill
 Supplement with Vitamin D, Calcium
and folic acid
 Interactions with Calcium Channel
Blockers, Antipsychotics and steroids
 P-450 = many interactions

106
 Anti-convulsant Drugs
 Interactions…
 Oral tube feedings with osmolite or isocal may
interfere with absorption of oral dilantin
diminishing drug’s effectiveness
 IV dilantin precipitates with D5W.
 Characteristics of fosphenytoin (Cerebyx) –
preferred over IV Dilantin
 Prodrug of phenytoin
 Rapidly converted by blood and liver
enzymes to phenytoin (Dilantin)
 Given I.V. only
107
 Anti-convulsant Drugs
Barbiturates and deoxybarbiturates
 Examples: Mephobarbital, phenobarbital, primidone
 Indications:
 Treat tonic-clonic seizures, partial seizures and
insomnia
 Used as adjuncts to anesthesia

 Adverse effects: Dizziness, drowsiness, hypotension,

respiratory depression with high doses
 Interactions: Drugs decreases serum dilantin level
when used concurrently
 Primidone plus phenobarbital may cause
phenobarbital toxicity

108
 Anti-convulsant Drugs
Benzodiazepines
 Examples: clonazepam (Klonopin) Diazepam
(Valium)
 Indications: treat absence seizures, status
epilepticus, anxiety and skeletal muscle
spasms.
 Adverse effects: ataxia, drug dependence,
respiratory and cardiovascular depression

109
 Valproic acid (Depakene)
Divalproex (Depakote)
 Low side effect profile, well tolerated
 May cause liver failure (rare) in first 6
months of therapy
 Lethargy, muscle weakness, sedation
 Leukopenia
 Ataxia
 Depakene causes nausea/vomiting
 Interacts with many other anticonvulsants

110
 Nursing Considerations
 Good for generalized and partial seizure
 Monitor blood levels
 Monitor CBC and liver function tests
 Highly protein bound, do not take with
NSAIDs, aspirin & other drugs that alter
coagulation
 Potentiates CNS depressants
 Reassure patient of alopecia, hair will re-
grow
 Used as mood stabilizer for bipolar disorder
and has FDA approval for this
111
 Carbamazepine (Tegretol)
 Blood dyscrasias
* Notify health care provider
 Liver toxicity
 Rash
 Drowsiness
 Low side effect profile – well tolerated
* Immediately discontinue & switch to another
agent

112
 Nursing Considerations
 Low behavioral and toxicologic profile
 Good for both generalized and partial
seizures
 Autoinduction – dosage needs monitoring
via blood levels, decreases after initial doses
 Advise alternate birth control if on pill
 Monitor CBC for bone marrow depression
 Used “off label” as mood stabilizer for
bipolar disorder

113
 Lamotrigine (Lamictal)
 Monotherapy in partial seizures
 Well tolerated
 No weight gain, no sedation
 Rare, but can be associated with life
threatening rash (Stevens-Johnson
syndrome)
 Nausea, vomiting, weight loss (rare)
 Dizziness, ataxia

114
 Nursing Considerations
 Discontinue at once if rash/inform health care
provider
 Nurse asks patient every visit
 Taper on very slowly to avoid rash – 25 mg Q 2
weeks until 200 mg
 No blood levels required
 Note many anticonvulsants raise or lower plasma
levels
 Monitor for adverse reactions if not monotherapy
 May reduce effectiveness of estrogen
 Used for mood disorder in bipolar, good for
depressive side, and has FDA approval for this
115
 Topiramate (Topamax)
 Adjunctive therapy in partial and generalized
seizures (studies support monotherapy)
 Well tolerated
 Fatigue
 Confusion
 Difficulty concentrating, speech problems
(unable to recall words)
 Nausea
 Weight loss
 No blood levels required

116
 Gabapentin (Neurontin)
 Adjunct therapy for partial seizures (studies
demonstrate monotherapy)
 Excellent side effect profile
 Main problem is initial sedation, ataxia
 Not metabolized by liver so no interactions with
other anticonvulsants
 Used extensively for neurogenic pain
 Excellent for elderly and those on poly drugs
 No blood levels required
 Used “off label” as mood stabilizer for bipolar
disorder but no FDA approval for this
117
 Other uses for
Anticonvulsants
 Mood stabilizers
 Migraine headache

 Neurological pain

 Chronic pain syndrome

 Anxiolytics

118
 Anti-Parkinsonian Drugs
Groups of Drugs Used

 Antidyskinetic Drugs or anticholinergics

 Antihistamines (have anticholinergic effects)
 Dopaminergics
Dopaminergicagonists
MAOI-B (monoamine oxidase inhibitor)

COMT Inhibitors (catechol-0-methyl-transferase)

119
 Anti-Parkinsonian Drugs
 Dopaminergic agonists are mainstay
 Contraindications and precautions:
 Used with caution in patients with residual
arrhythmias after MI, history of peptic ulcer,
psychosis or seizure disorders
 Contraindicated with narrow angle glaucoma
 Used with caution for patients with bronchial
asthma, emphysema, or severe cardiovascular,
pulmonary, renal, hepatic or endocrine disease
 Adverse Effects:
 Dizziness,
confusion, mood changes, orthostatic
hypotension, nausea, vomiting, hallucinations
120
 Anti-Parkinsonian Drugs
 General Information
 Mechanism of of action: Restore the natural balance of
the neurotransmitters in CNS to decrease S/S of
Parkinson’s Disease. Imbalance between Achetylcholine
(ACH) and Dopamine. Too much ACH and too little
dopamine. Meds correct this.
 Dopaminergic agonists
 Mechanism of Action is to increase the amount of DA
available in the CNS or enhance the neurotransmission of
Dopamine
 Medication examples:
 Levodopa restores dopamine levels
 Amantadine increases the amount of dopamine in the brain
 Pramipexole (Mirapex) – newer DA receptor agonist
 Ropinirole (Requip) – newer DA receptor agonist 121
 Anti-Parkinsonian Drugs
anticholinergics
 Drug examples: Benztropine (Cogentin)
 Trihexyphenidyl (Artane)
 Procyclidine (Kemadrin)
 Indications:
 Bradyarrhythmias, dyskinesia, parkinsonism, peptic ulcer and
bowel spasms
 Nausea, vomiting, induce mydriasis, decrease salivation and
bronchial secretions before surgery
 Contraindications:
 Narrow-angle glaucoma, severe hemorrhage, uncontrolled
tachycardia, urinary tract/GI obstruction, BPH
 Adverse effects:
 Blurred vision, conjunctivitis, and photophobia, tachycardia,
constipation, dry mouth and urinary hesitancy
 CAN CAUSE PSYCHOTIC CONFUSION IN THE ELDERLY
when drugs with anticholinergic effects are combined. 122
 Two Newer class to treat
Parkinsons
 Selegiline (Eldepryl)
MAOIB (monoamine oxidase inhibitor – B)
 May have neuroprotective effects slowing the
progression of the Disease
 Tolcapone (Tasmar) & entacapone (Comtan)
Catechol O-methyltransferase (COMT) inhibitors = newest class
 Not used as monotherapy, but as add on to levadopa
to increase its efficacy.
 Tasmar has been associated with liver dysfunction.

123
 Two classes that reduce
dosage of Levadopa
 MAOI-B DA in brain by inhibiting its
metabolism by MAO. Form “B” metabolizes
DA. At oral doses < 10mg Q.D. like MAOI- A
so acts more on tyramine NE, E, DA & 5H-T.
No food restrictions with low doses.

COMT inhibitors work by inhibiting the enzyme catechol-

O-methyltransferase the 2nd enzyme involved in the
metabolism of levodopa - so increased amount of levodopa
available.

124
 Wearing off syndrome

Doses need to be adjusted upward and

downward as adverse mental changes
occur or Parkinson’s symptoms worsen.
Changing doses is done slowly.

125
 Advanced Parkinson’s
A new DA agonist Apomorphine (Apokyn) given
S.Q. is available for advanced Parkinson’s as a
rescue drug for acute rigidity.
This is temporary add on, not replacement. N/V.
Rx for antiemetic.
Not 5-HT3 antagonists like ondansetron (Zofran)
because of hypotension.
Use trimethobenzamide (Tigan). Why do you
NOT want to use prochlorperazine
(Compazine)??

126
 Drugs used to Treat
Alzheimer’s
Cholinesterase inhibitors
 Increase Acetylcholine (Ach) in key areas of brain
(cerebral cortex)
 Reversible cholinesterase inhibitors
 Used to Treat mild to moderate disease
 Do not reverse symptoms; slow progression
 Check P450 for drug interactions
Examples
 Donepezil (Aricept)
 Tacrine (Cognex) (1st, most adverse effects, not used
today)
 Rivastigmine (Exelon) – newer {may have greater
efficiacy}
127
New class to Treat Alzheimer’s
 Memantine (Nameda)
 Released Jan. 2004 for Treatment of
moderate to severe Alzheimer’s Disease
 May have more favorable side effect
profile than Ach inhibitors
 May be possible to combine with ACh
inhibitors for better result

128
 Drugs Affecting the
Cardiovascular and Renal
Systems

Drugs to Treat:
Congestive heart failure
Hypertension
Angina
129
Inotropic (increase force of contraction)
Drugs and Cardiac Glycosides
 Indications
 Used to treat CHF in combination with other medications.
 Control ventricular rate in atrial fibrillation, atrial flutter,
paroxysmal atrial tachycardia
 Contraindications and precautions
 Uncontrolled ventricular arrhythmias, constrictive
pericarditis, complete heart block
 Increased risk of toxicity with hypercalcemia, hypokalemia,
hypomagnesemia, hypothyroidism, or renal failure
 Very narrow therapeutic index
 Elderly patients more sensitive to toxic drug effects
 Adverse effects – bradycardia, fatigue, weakness, nausea,
vomiting, diarrhea, visual disturbances
 Monitor pulse – hold if less than 60/min. apical
 Do not increase longevity in CHF
130
 Inotropic Drugs and Cardiac
Glycosides
 Interactions
 K-wasting diuretics and other drugs causing K loss increase
risk of toxicity
 Amiodarone, diflunisal, diltiazem, nifedipine, quinidine,
verapamil increase the serum drug level and may cause toxicity
 Concurrent use of beta adrenergic blocking drugs causes
additive bradycardia
 Antacids, cholestyramine, and colestipol decrease the
absorption of cardiac glycosides
 Digitalis preparations
 Examples: Digitoxin (long ½ life –not used often), digoxin
 Nursing responsibilities
 Digoxin excreted unchanged by the kidneys, dosage must
be reduce with renal impairment
 Monitor serum digoxin levels to prevent toxicity

 Digoxin Immune Fab IV to reverse toxicity

131
 Antihypertensive Drugs
 Antihypertensive drugs
 Indications
 HTN not controlled by life style modifications
 Classes
 Beta-adrenergic blocking drugs, angiotensin-
converting enzymes (ACE) Inhibitors, angiotensin-
receptor blockers,(ARB’s), calcium channel
blockers, alpha 1 blockers, centrally acting alpha 2
agonists, diuretics, peripheral acting vasodilators
 Contraindications and precautions
 Each class has own action, side effects, specific
recommendations and adverse reactions
132
 Antihypertensive Drugs
2nd line agent
 Peripheral vasodilating drugs
 Drug examples: hydralazine
 Mechanism of action: exert direct action on both
arteries and veins to decrease peripheral vascular
resistance (with beta blockers)
 Indications: treatment for hypertension and
hypertensive crisis
 Adverse effects: fluid retention, tachycardia,
orthostatic hypotension, severe hypotension and
nausea
 Nursing responsibilities
 Closely monitor for fluid volume excess
 Rarely used

133
 Antihypertensive Drugs
 ACE Inhibitors (1st line agent)
 Drug examples: benazepril, catopril, enalapril, fosinopril, lisinopril
 Mechanism of action: block conversion of angiotensin I to
angiotensin II
 Mode of Action
 Vasodilation due to inhibition of Renin Angiotension Aldosterone
system, decreased blood volume due to decreased (Sodium) Na+
 Adverse effects: dizziness, light-headedness, fainting, tachycardia,
palpitations, rash, proteinuria
 Nursing responsibilities
Not effective with African Americans
 Do not give with Na+ sparing diuretics
 Monitor for dry cough
 Contraindicated in pregnancy and renal stenosis
 Not to be given with lithium and caution with NSAIDs
 Indications: HTN, CHF, diabetes, Angina

134
 Antihypertensive Drugs
 Calcium channel blockers (1st line agent)
 Drug examples:
 Amlodipine, diltiazem, felodipine, verapamil, nifedipine
 Mechanism of action:
 Dilate vessels by blocking the slow channel, preventing calcium
from entering the cell
 Adverse effects:
 Grapefruit juice can cause toxic overdose
 Dizziness, AV blocks, headache, edema, flushing, nausea,
constipation, bradycardia
 P-450 interaction with other meds
 Do not give with grapefruit juice- can cause toxic overdose
 Nursing responsibilities
 Watch for weight gain if CHF
 Indications: Angina, arrhythmias, HTN
135
 Antihypertensive Drugs

 Diuretics – thiazide (1st line agent)

 Drug examples: chlorothiazide, hydrochlorothiazide
 Mechanism of action: inhibit sodium and chloride
reabsorption, distal tubule, reduce blood volume
 Adverse effects:
 Fatigue, dizziness, orthostatic hypotension, rash,
hypokalemia, hyperglycemia
 Indications: 1st line for HTN, take in the morning

 Diuretics – loop
 Mechanism of action: Loop of Henley, reduce blood
volume example: furosemide (Lasix)
 Adverse effects: electrolytes
 Indications: CHF 136
Antihypertensive Drugs
Selective Beta Blockers – 1st line agent
 Drug examples: Atenolol
 Mechanism of action: Selectively block beta 1 receptors in
the heart so slows heart rate – chronotropic effect and –
inotropic effect
 Adverse effects: Bradycardia, rebound HTN if abruptly
stopped, fatigue, dizziness, dyspnea
 Indications: HTN, Prophylaxis for angina, CHF, post M.I.
for cardioprotective effects
 Nursing responsibilities: Monitor pulse, watch for drug
interactions (CCBs), potentiated by alcohol and other CNS
depressants, give cautiously with asthma patients
137
 Antihypertensive Drugs

 Angiotensin-receptor blockers
 Alpha 1 blockers

 Centrally acting alpha 2 agonists

All 2nd line agents

138
 Antianginal Drugs
 Mechanism of action:
 Reduce myocardial oxygen demand or increase coronary
blood supply
 Indication:
 Angina pectoris
 Contraindications:
 Hypotension, uncorrected hypovolemia
 Adverse effects:
 Flushing, headache, orthostatic hypotension
 Interactions:
 Produce additive hypotension when used with alcohol,
antihypertensives, beta-adrenergic blocking drugs or
calcium channel blocker drugs for erectile dysfunction.139
 Antianginal Drugs
 Nitrates
 Drug examples:
 Erythrityltetranitrate, isosorbide dinitrate (Isordil)
Nitroglycerin, Nitro-BID
 Mechanism of action:
 Produce vasodilation. Decrease preload and
afterload, and reduce myocardial oxygen
consumption
 Indications:
 Management of angina, and chronic anginal attacks
 Beta Blockers and Calcium Channel Blockers also
for long term management

140
 Diuretic Drugs
 Thiazide and thiazide like diuretics
 Drug examples: Clorothiazide, hydrochlorothiazide
 Mechanism of action: Increase sodium and water
excretion by inhibiting sodium reabsorption in the
distal tubule of the kidney
 Contraindications: Sensitivity to sulfonamides
 Adverse effects: Hypokalemia, hyperglycemia,
arrhythmias, orthostatic hypotension, weakness, muscle
cramps, photosensitivity reactions
 Interactions:
 Decrease excretion of lithium causing toxicity
 Concurrent use with other K-depleting drugs and cardiac
glycosides may cause low K and risk of digitalis toxicity
 NSAID may reduce response to thiazide diuretics
 Do not take if allergic to sulfa drugs 141
 Diuretic Drugs
 Loop diuretics
 Drug examples:
 Bumetanide (bumex) ethacrynic acid, lasix, torsemide
 Mechanism of action:
 Inhibit
sodium and chloride reabsorption from the
loop of Henle and the distal tubule
 Adverse effects:
 Metabolicalkalosis, hypovolemia, dehydration.
Hyponatremia, hypokalemia, hypochloremia,
hypomagnesemia, photosensitivity, orthostatic
hypotension

142
 Diuretic Drugs
 K-sparing diuretics
 Drug examples:
 Amiloride, spironolactone, triamterene
 Mechanism of action:
 Act at the distal tubule to cause excretion of sodium,
bicarbonate, and calcium and conservation of K
 Adverse effects:
 Hyperkalemia, nausea, vomiting, diarrhea
 Interactions:
 Decrease excretion of lithium
 Concurrent use with ACE inhibitors or K increases risk
of hyperkalemia
 NSAIDs may reduce the effects of K sparing diuretics.
 Give cautiously with renal insufficiency patients
143
 Diuretic Drugs
 Osmotic diuretics
 Drug examples:
 Mannitol, Urea
 Mechanism of action:
 Increase osmotic pressure of the glomerular
filtrate inhibiting reabsorption of water and
electrolytes
 Osmotic diuretics create an osmotic gradient in
the glomerular filtrate and the blood
 Adverse Effects:
 Hyponatremia, dehydration, circulatory overload,
rebound IICP
144
 Antilipemics
WE EAT TOO MUCH FAT
in the typical American diet.

DRUGS TO LOWER CHOLESTEROL:

VDRL, LDL and TGs
 Syndrome X
metabolic syndrome
Glucose intolerance
Insulin resistance
Hypertension
Dyslipidemia
Hypertriglyceridemia
Associated with Male-shaped obesity
Cardiac Disease
Female hip-to-waist ratio
146
 Classes that lower lipids

 HMG-CoA Reductase Inhibitors or

Statins
 Nicotinic Acid

 Fibric Acid Derivatives

 Cholesterol Absorption Inhibitors

•Bile Acid Sequestrants

147
 Anticoagulant, antiplatelet
and thrombolytic drugs
 Anticoagulant drugs prevent extension and
formation of clots by inhibiting factors in
the clotting cascade
 Thrombolytic drugs activate plasminogen,
leading to its conversion to plasmin
 Antiplatelet drugs interfere with platelet
aggregation, preventing thromboembolic
events

148
 Common Pathway
Vit. K + warfarin Factor X Low molecular
weight heparin
Prothrombin
Heparin +
antithrombin = (factor II)
Activated Heparin
Thrombin

Fibrinogen
Thrombolytics
Fibrin clot

Clot plasmin plasminogen

Photo Source: Used courtesy of E. McCabe,
RN, Santa Barbara City College dissolves 149
 Anticoagulants
 Examples: Dalteparin, enoxaparin, heparin, warfarin
 Indications: prevent and treat thromboembolic
disorders such as DVT, PE, and atrial fibrillation
with embolization
 Adverse effects: thrombocytopenia (with heparin)
 Androgens, chloral hydrate, chloramphenical,
metronidazone, quinidine, sulfonamides, thrombolytic
drugs, and valproic acid increase the risk of bleeding
and enhance the effects of coumadin
 Alcohol, barbiturates, estrogen-containing oral
contraceptives and foods high in Vitamin K increase
risk of clotting and may decrease effect of heparin
150
 Heparin
 Accidentally discovered by medical student
in 1916, used medically first time in 1935 on
humans
 High molecular weight – called
unfractionated
 Does not cross the blood brain barrier – can
be used during pregnancy
 Half life IV = 45 to 90 minutes
 Half life SQ = 60 to 120 minutes
 Bioavailabity is about 20 to 30 %
151
 Heparin
 Destroyed by enzymes in the GI tract
 Administered IV or SQ – IM = muscular
hematomas
 Varying bioavailability
 Monitor with - aPTT (activated partial
thromboplastin time) =
 Preferred because more sensitive to intrinsic
pathway

152
 Heparin
Highly protein bound = variable anticoagulation b/c
the ill have reactive proteins that also bind to heparin.
 Most serious side effect is hemorrhage
 Administer protamine sulfate by slow IV infusion to neutralize
heparin
 Drug-drug interactions: antiplatelet drugs, NSAIDs oral
anticoagulants, nitroglycerin, cephalosporins, penicillins,
salicylates all may affect of heparin
 Uses: Hemodialysis, open-heart surgery, prevention of
thromboembolism, post MI, inhibits platelets from binding, DVT,
PE, atrial fib, stroke prevention a.k.a. acute brain attack or CVA

153
 Anticoagulants
 Nursing Responsibilities
 Heparin given initially because of its rapid
action, then switch to coumadin over several
days until therapeutic level is reached
 Heparin affects PTT and coumadin PT
 Inject SQ in abdomen and do not aspirate or
rub at injection site
 Protamine sulfate antidote for heparin
 Vitamin K antidote for coumadin
 Soft toothbrush and electric razor

154
 Anticoagulants
 Monitoring heparin therapy
 Obtain baseline PTT
 Administer a bolus dose of heparin IV, as ordered
 Follow with continuous infusion as ordered
 Obtain follow up PTT at specified
 Values> 1 ½ time the control
 Continue to monitor
 Assess for S/S of bleeding
 Values < 1 ½ time the control
 Contact MD
 Anticipate dosage increase
 Increase dosage as ordered

155
Low molecular wt. Heparin
example enoxaparin (Lovenox)

 Given by SQ injection
 Mainly Acts on factor X to begin the
coagulation cascade to inhibit the
conversion of prothrombin to thrombin.
Produces greater prothrombin effect than
binding to factor II as Heparin does.
 Also called fractionated heparin

156
 Low Molecular wt. Heparin
 T.I.A.s
 Ischemic symptoms
 Unstable angina
 Atherosclerosis
 Non ST elevation M.I. a.k.a, Q wave M.I.
(without elevated enzymes - homocystine)
 ST elevations a.k.a. acute M.I. (with elevated
enzymes- homocystine)
157
 Low molecular wt. Heparin

 High bioavailability and so more predictable

than heparin because binds to factor X
 No routine testing required
 Can be administered at home
 Bleeding is main adverse effect
 Usually weaned off and when stable onto
warfarin (Coumadin)

158
 Oral anticoagulant
Warfarin (Coumadin)
 AKA “rat poison”
 May also be given IV, but rarely is
 Bound tightly to plasma protein – other drugs
can displace + other proteins may be present
during tissue breakdown (example C- reactive
protein)
 Very difficult to monitor PT (prothrombin
time) and dosed by INR (international
normalized ratio)
 Long half- life 1 to 3 days
159
 Warfarin (Coumadin)

 Variable dosing and unpredictable; MUST COME IN

FOR FREQUENT MONITORING.
 Used prophylaxis for deep vein thrombosis (DVT),
Pulmonary Embolus (PE), atrial fibrillation, off label
for recurrent Transient Ischemic Attack (TIA),
recurrent Myocardial Infarction (MI)
 Suppresses coagulation activity by interfering with
the production of vitamin K-dependent clotting
factors in the liver.
 Reduced amount of available Vitamin K for clotting
factors II, VII, IX and X
160
 Warfarin (Coumadin)
 Humans can not synthesize Vitamin K, but
bacteria in GI tract can
 Treat excessive bleeding with Vitamin K
 Watch for bruising
 Careful in older adult because MANY drug
interactions and fall can cause excessive bleeding
 Used to prevent clot formation in conditions such
as atrial fib, not acute situations
 IV Heparin to PO warfarin administer the 2
drugs simultaneously for 2 to 3 days to ensure
continuous therapeutic anticoagulation
161
 Antiplatelets
Clopidogel (Plavix) & ticlopidine (Ticlid) bind to
ADP (adenosine dephosphate) which inhibits its
effect on platelets (60 – 70% )
Aspirin inhibits thromboxane (TX2) in
Arachidonic Acid Pathway (30-40%)
Abciximab (ReoPro) binds to the GP IIb/IIIa
receptor and inhibits platelet aggregation (90%)
Tirofiban (Aggrastat) {new}

162
 Antiplatelet Drugs
 Drug examples:
 Aspirin, dipyridamole (persantine), Ticlopidine (Ticlid)
 Indications for use:
 Prophylaxis for thrombo-embolic events
 Ticlid – second line drug use to prevent stroke in high
risk individuals, decrease intermittent claudication, and
decrease graft occlusion after coronary artery bypass
 Contraindications:
 Active bleeding, thrombocytopenia, severe liver
impairment
 Adverse effects: Bleeding, tinnitus, dizziness, neutropenia
(Ticlid)

163
 Thrombolytic Drugs
 Drug examples:
 Alteplase (tissue plasminogen activator)
(activase), streptokinase, urokinase
 Indications for use:
 Drugs used to lysis coronary artery thrombi
 Alteplase, streptokinase, and urokinase used to
treat PE
 Streptokinase and urokinase used to treat DVT
and to clear arterial catheters and arteriovenous
shunt
 MRI needed for CVA to determine cause
164
 Thrombolytic Drugs
 Contraindications: Recent streptococcal
infection, active internal bleeding
 Adverse effects: urticaria, fever
 Nursing responsibilities:
 Monitor V/S for bleeding or hypotension, check
peripheral pulses to ensure circulation
 Keep typed and cross matched blood on hand to
administer in case of hemorrhage
 Thrombolytic drugs should be administered only when
the patient’s hematologic function and clinical
response can be monitored
 Ensure that aminocaproic acid (Amicar), the antidote
for thrombolytic overdose, is readily available
165
 Antiplatelet Drugs
 Drug examples:
 Aspirin, dipyridamole (persantine), Ticlopidine (Ticlid)
 Indications for use:
 Prophylaxis for thrombo-embolic events
 Ticlid – second line drug use to prevent stroke in high
risk individuals, decrease intermittent claudication, and
decrease graft occlusion after coronary artery bypass
 Contraindications:
Active bleeding, thrombocytopenia, severe liver
impairment
 Adverse effects: Bleeding, tinnitus, dizzines,
neutropenia (ticlid)

166
Drugs Affecting the
Endocrine System

167
 Thyroid Hormones
 Thyroid replacement increases metabolism,
cardiac output, regulates cell growth and
causes diuresis.
 Most commonly used: – thyroid and levothyroxine
(Synthroid)
 Contraindications: – Recent MI, adrenal
insufficiency, hyperthyroidism
 Side Effects: – Cardiac dysrhythmias
 Adverse Effects: – Tachycardia, angina, hypertension,
insomnia, headache, anxiety, increased or decreased
appetite, menstrual irregularities, weight loss, heat
intolerance (“hot flashes”) and thyroid storm
168
 Antithyroid Drugs
 Used to treat hyperthyroidism
 Most commonly used: – methimazole and
propylthiouracil which inhibit formation of thyroid
hormone
 Contraindication: – Drug allergy, avoid in pregnancy if
at all possible
 Side Effects: – Drowsiness, smoky colored urine, aching
 Adverse Effects: – Increased BUN and creatinine,
enlarged thyroid, liver and bone marrow toxicity
 Interactions:– Increase in activity of anticoagulants
 Propranolol (Inderal) (non-selective beta blocker) given to
control symptoms before antithyroid drugs work 2-3
weeks
169
 Insulin
 Replaces insulin not made or made
defectively in the body.
 Indicated primarily for Type I diabetes but may be
used with Type II
 Requires careful dosing regimen
 Contraindications: – Drug allergy to specific product.
 Adverse Effect: – Hypoglycemia from overdose,
weight gain
 Interactions: – corticosteroids, epinephrine,
furosemide, phenytoin, thiazides, thyroid hormones,
alcohol, anabolic steroids, MAO inhibitors
170
 Action of Insulins
Preparation Onset of Action Peak Action Duration of
Action
30-60
Humalog 10-15 minutes minutes 5 hours or less

Regular* 30-60 min 2-4 hrs 6-10 hrs

NPH/Lente 1-2 hrs 4-8 hrs 10-18 hrs

Ultralente 2-4 hrs 8-14 hrs 18-24 hrs

Insulin glargine (Lantus) - a basal insulin for tighter glycemic control.
Do not mix with insulin. May be used also for type 2 glycemic control.
Regular insulin can be given IV in emergency situations
171
 Sliding Scale (Rainbow Coverage)
 Regular insulin is given according to blood
glucose results.
 Used mostly with newly diagnosed diabetics when
stress occurs, such as illnesses requiring
hospitalization and surgery
 Used with blood glucose greater than 200 mg/dl
 Example:
 4 units = 200 – 250
 6 units = 251 – 300
 8 units = Greater than 300
 May need to call MD – Carefully check order.
172
Classes of agents for Type 2

 SULFONYLUREAS
 1ST generation
 2nd generation
 ALPHA-GLUCOSIDASE INHIBITORS
 BIGUANIDES
 MEGLITINDES
 THIAZOLIDINEDIONES
 INCRETIN MIMETICS (injected, new for type 2)
 SYNTHETIC ANALOGS OF AMYLIN (injected,
new (1 & 2)
 Insulin glargine for tighter control (1 & 2)
 Inhaled insulin (1 & 2) “EXTRA, EXTRA!
Two new
classes!”
173
Complications of uncontrolled
Type 2
 Vascular disease especially hypertension
 Urinary Tract Infections (UTIs)

 Vaginitis

 Prostatitis

 Retinopathy

 Nephropathy

 Nonketotic coma (uncontrolled)

174
 Sulfonylureas (secretagogues)- means
stimulates the secretion of insulin

 First generation  Second generation

 EXAMPLE=Diabinese  EXAMPLE=
(chlorpropamide) Diabeta (glyburide)
 Potentiated by NSAIDs  Much the same as 1st
 Highly protein bound generation
 P450 system so drug  May increase insulin
interactions sensitivity
 Hypoglycemia  Also potential
 Stimulates pancreas hypoglycemia
 May increase incidence of
increased glucose intolerance
 Rarely used today 175
 Biguanides
 EXAMPLES
 Metformin (Glucophage XR) &
 Metformin (Fortamet XR)
 Action
 Decrease hepatic glucose production
 Increases insulin sensitivity
 Decreases intestinal absorption of glucose
 Improves lipid profile, decreases Triglycerides
 DOES NOT produce hypoglycemia
 Used as monotherapy or combination therapy
176
 Biguanides

New use as prevention of Type II with FBS <

110 mg/dL > 125 mg/dL & History in family
May lower vitamin B12 levels ? Best to
supplement

Side effects: Usually good side effect profile, GI

symptoms, WEIGHT REDUCTION
Do not give to patients who are being treated for
CHF because of possibility of lactic-acidosis

177
 Alpha-Glucosidase
Inhibitors
 EXAMPLES
 Acarbose (Pecose)
 Miglitol (Glyset)
 Action:
 Blocks intestinal amylase so delays breakdown
of complex carbohydrates
 Decreases postprandial glucose
 Monotherapy or combination therapy
 Side effects: are minimal - flatulence, diarrhea,
abdominal cramps
178
 Thiazolidinediones
 EXAMPLES
 Pioglitazone (Actos)
 Rosiglitazone (Avandia)
 Action:
 Reduce insulin resistance
 Monotherapy or combination with
sulfonylureas, metformin
 Enhance insulin action in skeletal muscle, liver
and fat tissue
 Reduce hepatic glucose output
 Glucose uptake into peripheral tissue
179
 Thiazolidinediones
 Precautions:
 Do not use in patients with hepatic dysfunction
 Monitor liver function tests
 Caution with cardiac patients
 In combination with other antidiabetic agents,
can cause fluid retention, may exacerbate CHF;
caution with insulin use
 Side effects:
 May cause edema and weight gain, headache,
upper respiratory infection
 Does not cause hypoglycemia when used as
monotherapy
180
 Meglitinides
(partial secretagogues)

 EXAMPLES
 Repaglidine (Prandin)
 Taken ½ hour before meals
 Rapidly absorbed
 Needs presence of glucose to exert it’s action
 Stimulates release of insulin
 Side effects:
 Potential for hypoglycemia, URI
 Monotherapy or combination with metformin
181
 Amino Acid Derivative
a secretagogue

 EXAMPLE
 Naeglinide (Starlix)
 Give adjunct with diet & exercise
 Give to those who have not been treated
chronically with other antidiabetic agents
 Take 1 hr. to 30 min. before meals
 Caution if patient is malnourished
 Skip dose if meal skipped
 Contraindicated in Type I and ketoacidosis
 Not recommended in pregnancy
 Monitor when concurrent highly protein-bound
drug given 182
183
Parathyroid hormone (PTH)
 Stimulated by low serum calcium
 Inhibited by normal or high levels of
calcium via negative feedback system
 Phosphate also regulated by PTH via an
inverse relationship with calcium
 PTH activates Vitamin D which increases
intestinal absorption
 Less urinary excretion of calcium
 Bone reabsorption of calcium from bone

184
Calcitonin & decreased PTH
 Hypercalcemia decreases secretion of PTH
 Calcitonin is synthesized in the thyroid
 Calcium is lost in urine
 Decreased absorption of calcium from the
intestine
 Decreased reabsorption of calcium from bone

185
 Vitamin D
 In activated form acts like hormone (intermediate
metabolism in liver then to active form in kidney
called calcitriol)
 Obtained from foods and by sunlight on skin
 Deficiency limits amount of calcium absorbed from
diet
 Causes release of calcium from the bone
(reabsorption)
 Causes G.I. absorption of calcium
 Decreased levels caused by medications including
tetracyclines and Dilantin
186
 Osteoporosis
 Risk factors
 Current low bone mass (DXA) [dual energy x-ray
absorptiometry]
 Thin, small frame female
 Advancing age
 Family history of osteoporosis
 Estrogen/testosterone deficiency
 Anorexia nervosa
 Low lifetime calcium intake
 History of fracture after age 50
 Smoking, alcohol and sedentary life style
 Use of oral glucocorticoids for chronic disease
187
Drugs used for Calcium/bone Disorders
(osteoporosis & osteopenia)
 Biphosphonates: alendronate (Fosamax), risedronate
(Actonel) new once a month ibandronate (Boniva)
used for osteopenia, osteoporosis, Paget’s disease
 Action: undergo incorporation into bone.
Osteoclasts begin to reabsorb biphosphonate-
containing bone so they ingest some of the drug,
which then acts to inhibit their activity
 All poorly absorbed from GI tract.
 Take in a.m. with full glass of water, but without
food for 30 minutes and remain in upright position
to minimize risk of esophagitis.
188
Drugs used for Calcium/bone Disorders
(osteoporosis & osteopenia)

 Thyroid hormone: Calcitonin (Miacalcin)

• Produced by body when low levels of calcium
• Used to treat osteopenia
• Nasal spray
• Suppresses bone reabsorption
• Main side effect is runny nose and sneezing
• Hormone Replacement Therapy

189
Mechanisms that raise
serum calcium levels

If decreased Serum Calcium

Parathyroid hormone secretion
renal excretion of calcium
Intestinal absorption of
calcium via activation of Vit D
Bone resorption so calcium

190
Mechanisms that lower
serum calcium levels

If increased Serum calcium

Parathyroid hormone secretion
Calcitonin secretion
Renal excretion of calcium
Intestinal absorption of calcium
Bone resorption
Serum calcium 191
 Arthritis
Osteoarthritis Rheummatoid Acute gouty
arthritis (RA) arthritis
Excessive wear Autoimmune Uric acid crystals
& tear of wt. disorder with accumulate in
bearing joints autoantibodies joints
(rheumatoid
factors)
Often thought as Systemic Sudden onset,
normal part of manifestations triggered by diet,
aging process injury/stress;
often big toe
192
 Corticosteroids
 There are 2 types – Glucocorticoids and
Mineralcorticoids
 Cortisol is primary glucocorticoid
 Aldosterone is primary mineralcorticoid
 Some Indications:
 Replacement therapy for Addison’s Disease
 Inflammatory diseases
 Arthritis

 Ulcerative Colitis

 Nephrotic syndrome

 Liver disorders

 Ocular inflammations
193
 Corticosteroids (cont’d)
o Some indications: (cont’d)
o Allergic conditions – status asthmaticus,
asthma, allergic reactions
o Neoplastic diseases
o Brain-injuries (cerebral edema)
o Skin conditions (psoriasis/dermatitis)
o Collagen disease (Lupus)
o Ophthalmic – conjunctivitis, corneal
abrasions
o Asthma
194
 Corticosteroids (cont’d)
 Precautions:
 Therapy is tapered and not discontinued abruptly
 Vaccinations are contraindicated
 Use with caution during pregnancy, lactation, clients
high risk for infections, peptic ulcer disease (PUD),
cardiac or renal failure, diabetes, myasthenia gravis
 Do not use with fungal or viral eye infections
 Interactions – Increased risk of:
 Hypokalemia with K-depleting diuretics
 Digitalis toxicity
 Gastric ulcers with NSAIDS
 Hyperglycemia
195
 Estrogen
 Indications:
 Hormone replacement therapy
 Normal sexual development with estrogen deficiency
 Androgen suppression with prostate Ca
 Oral contraception by inhibiting ovulation
 Side Effects:
 Headache
 Depression
 Adverse Effects:
 Hypertension
 Thrombo-embolic disorders
 Abnormal uterine bleeding
 Unopposed may lead to endometrial cancer
196
 Estrogen (cont’d)
 Contraindications:
 Pregnancy and lactation
 Previous or active thrombo-phlebitis or embolic
disorders
 Estrogen-dependent Cancers
 History of CVA or Coronary Artery Disease (CAD),
Breast Cancer, liver disorders
 Precautions:
Oral contraceptives by diabetics or smokers
 Interactions: Some anti-convulsants decrease the
effectives of oral contraceptives due to P450 system
197
 Progentins
(not progesterone)

 Indications - Oral contraception with estrogen,

HRT, endometriosis, dysmenorrhea, uterine bleeding
 Adverse Effects:
 Breakthrough bleeding
 Impaired glucose tolerance
 Depression
 Edema and weight gain
 Contraindications:
 Pregnancy, undiagnosed vaginal bleeding,
Thrombo- phlebitic or embolic disorders, Ca of
reproductive organs
198
 Androgens
 Most important is testosterone
 Uses:
 Males – erectile dysfunction, delayed puberty, muscle
wasting in AIDS
 Females – Endometriosis, fibrocystic breast changes,
some menopausal symptoms, advanced breast cancer
 Females – increases libido
 Adverse Effects:
 Virilization, hepatotoxicity, edema, gynecomastia in
males
199
 Androgens (cont’d )
 Precautions:
 Contraindicated in pregnancy and prostate
enlargement
 Children must have bone growth evaluated q 6
months
 Anabolic Steroids – Schedule III controlled
substance (not same as testosterone)
 Testosterone
 Interactions:
 Enhance effects of oral anticoagulants, oral
hypoglycemics and insulin
 Barbiturates and calcitonin interfere with the effects
of androgens
200
Drugs Affecting the
Respiratory System

Photo Source: National Cancer Society, Public Domain,

http://visualsonline.cancer.gov/details.cfm?imageid=1775
201
 Antihistamines
 Indications:
 Various allergic reactions
 Induce sleep
 Relieve nausea
 Prevent motion sickness
 Side Effects:
 Drowsiness
 Dry mouth and blurred vision
 Elderly are at high risk for dizziness,
confusion, hypotension, unsteady gait &
CNS stimulation - Lower doses due to
anticholinergic effects 202
 Antihistamines (cont’d)
 Adverse Reactions:
 Headache, hypertension, GI distress
 Drug allergy – anaphylaxis
 Excessive sedation with other CNS depressants
 Contraindications:
 Narrow angle glaucoma, prostatic hypertrophy,
pregnancy, bladder neck obstruction, PUD
 Not recommended in bronchitis or pneumonia because
they dry secretions making it difficult for removal.
 Interactions:
 Some antibiotics enhance effects
 MAOIs inhibit metabolism thus enhancing effects 203
 Mode of Action Antitussives

narcotic antitussives directly

suppress cough reflex in
medulla of the brain (CNS)

dextromethorphan same
mode of action as narcotic

benzonatate anesthetizes or
numbs the cough reflex
Photo Source: Wikimedia Commons, Creative Commons,
http://commons.wikimedia.org/wiki/Image:Brain_bulbar_region.sv
g

204
 Antitussives
 Used to relieve coughs: suppresses cough center in
medulla if centrally acting
 Antitussives containing codeine are Schedule IV meds.
Dextromethorphan, non-opioid
 Side Effects for centrally acting:
 Drowsiness, sedation, dizziness, restlessness,
agitation, euphoria
 Adverse Effects:
 Respiratory depression – antidote opioid toxicity
(Narcan)
 Hypotension, Tachy or bradycardia
 Drug allergy - Anaphylaxis
205
Drugs Affecting the Respiratory
System
 Beta-Agonists inhaled - short acting +
long acting
 Beta-agonists – oral agents
 Methylxanthines
 Anticholinergics
 Antiasthmatics
 [cromolyn & nedocromil]
 Corticosteroids
 Leukotriene modifiers
206
 Bronchodilators
 Used to relax smooth muscles in bronchi and
bronchioles for asthma, bronchitis,
emphysema
 3 Types of Drugs
 Adrenergics(beta -2)
 Xanthines

 Anticholinergics
(given by inhalation)

207
 Follow step approach guidelines when doing
health teaching.
 See health care provider at least every 6
months for evaluation.
 Identify and list triggers.
 Keep asthma diary & record “personal best”
from peakflow meter. Record three times a
day.
 Contact provider if peak flow drops and go to
established plan. 208
Step Approach Terms
 Step one
 Mild Intermittent
 Step Two
 Mild Persistent
 Step Three
 Moderate Persistent
 Step Four
 Severe Persistent

209
 Beta-Agonists
Rescue drugs (short acting)

 Used most often

 During acute phase of asthmatic attack
 For COPD acute attack of SOB
 Quickly reduce airway constriction
 Are Sympathomimetics
 Stimulate beta-2 receptors

210
 Anticholinergics
Corticosteroids
Indirect-acting Agents
211
 Anticholinergics
Controller drugs
 Ipratropium bromide = Atrovent
 New powder inhaler (not metered dose inhaler)
24 hr. duration & may be superior to atrovent =
tiotropium bromide (Spiriva)
 NOT for acute attacks!
 For maintenance tx of bronchospasms
 MAINSTAY FOR COPD (when combined with
atrovent is called Combvient – brand name)

212
 Side Effects of Anticholinergics

 Respiratory:
 Dry mouth or throat and coughing
 Gastrointestinal:
 GI distress
 CNS:
 Headache & anxiety

Mild anticholinergic effects if inhaled – do not use if

patient has glaucoma or BPH
Atrovent or Combivent inhalers produce serious
allergic reactions to those with peanut allergy
213
 Xanthine Bronchodilators
Controller agent

 Aminophylline *usually I.V. when patient

in distress
 Theophylline *[examples]
 aerolate, bronkodyl, elixophyllin, slo-bid,
theobid, theo-dur, theolair, & uniphyl

214
 Theophylline
 Wide variability as to plasma half-life
 Narrow therapeutic index
 Unpleasant side effects of anxiety, agitation,
insomnia, tachycardia, palpitations
 Need to draw blood samples to stabilize patient
on correct dosage to minimize adverse effects
 Older adults with liver disease and CHF with
pulmonary edema have prolonged half-life
 Smokers and children have shorter half-life

215
 Antibiotic classes:
Sulfonamides, Penicillins,
Cephalosporins, Macrolides,
Quinolones, Aminoglycosides,
Tetracyclines, Glycycyclines
Carbapenems,
Monobactams, Oxazolidinones
Streptogramins, Ketolides &
Glycylcyclines
216
 Drugs Used to Treat
Infections
 Drugs for treating infections are referred
to as antibiotics (most common term) or
anti-infectives, antimicrobial
 Antibiotics are not effective against
viruses
 Resistance is the BIG PROBLEM

217
 Anti-infectives General Action

Modifies
protein Damages
synthesis the cell wall
Types of
antibiotic action
Modifies
Modifies energy
DNA metabolism
synthesis via folic acid

218
 Antibiotics
Actions
 Inhibit the growth of bacteria
 Inhibit cell wall synthesis
 Are bacteriostatitic and bacteriocidal
 Adverse Reactions:
 Some are very nephrotoxic
 Hearing impairment- ototoxic
 Superinfections
 May potentiate decreased effectiveness of other medications
(Be aware of specific interactions with specific drugs)
 “Sunburn” reaction – Avoid direct sunlight with tetracyclines
 Contraindications:
 Known drug allergy
 Many should not be used during pregnancy
 Many resistance patterns 219
 Penicillin resistance
 Penicillinases (enzymes) produced by
bacteria that destroy penicillin by
cleaving the beta-lactam ring of the drug
 Clavulanic acid enhances the activity of
penicillins. Binds to the active sites of
penicillinases rendering the enzyme
inactive

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 Some Commonly Used
Antibiotics
 Sulfonamides
 One of the first anti-infectives
 Often used today for Urinary Tract Infections
 Drink fluids to prevent urinary crystals
Septra
 Bactrim

 Assess allergy to other sulfa medications

(Sulfonylureas,Thiazide diuretics)
 Penicillins
 Penicillin G, Ampicillin, Amoxicillin
 Observe for clostridium difficule
 Fruit juices can inactivate the drug
 Assess electrolytes 221
 Some Commonly Used
Antibiotics (cont’d)
 Tetracyclines (not with milk, CA products)
 Take one hour before or two hours after meal
 Causes brown teeth in children!
 Photosensitivity
 Macrolides – Erythromycin and Biaxin can have
many drug interactions, problems with G.I. distress
 Used to treat mycoplasma (penicillins &
cephalosporins not effective!)
 Used when patient is allergic to penicillin
 Use cautiously with heart, renal, liver disease
 Not given with fruit juice
222
 Cephalosporins
• Similar to PCN but broader spectrum
• Differ as to generation for coverage. When
anaphylaxic reaction to PCN, should not be
given a cephalosporin
• A beta-Lactam antibiotic
• May be ineffective against bacteria that
produce
enzyme beta-lactamase
• Called cephalosporinase
• Avoid alcohol. Also, now may not be effective 223
 Quinolones
 Kill bacteria = bactericidal
 Active on a wide variety of bacteria
 gm- & gm+ as well as a-typical infections
 Excellent oral absorption
 Antacids reduce their absorption
 * gm- coverage & excellent [drug] for kidneys
 Great for treating UTI’s & prostatitis first oral class
of antibiotic to kill gram- bugs
 Good for Salmonella typhi and Shigella
 Not used in children. May damage cartilage, leading
to deformities in gait
224
 Quinolones

 Used to treat:
 lower respiratory tract infections
 bone & joint infections
 infectious diarrhea
 urinary tract infections
 skin infections
 Overuse! They should be reserved for serious
infections and resistant strains. MRSA can be
susceptible. Do not want to create resistance
 Should not be used in children - may damage
cartilage leading to deformities in gait
225
 Aminoglycosides
Used to Treat:
Pneumonias, resistant UTIs, septicemia, CNS
infections – serious & life threatening
Action:
Bind to 30S & 50S ribosomal subunits
Cause inhibition of protein synthesis
Precautions:
Nephrotoxicity & ototoxicity (8th cranial nerve)
Drug levels help prevent high peaks & troughs,
many drug interactions; must monitor carefully.
226
 Miscellaneous antibiotics
 Vancomycin
 Rapidly bactericidal so low resistance
 Glycopeptide antibiotic not related to PCNs
 Given by intermittent IV infusion
 Used in life-threatening staph or strep infections and
MRSA
 Adverse reactions are nausea, flushing and itching
 Red Man Syndrome

 Toxic reactions: tinnitus, hearing loss,

nephrotoxicity
 Often given with piperacillin (Zosyn) IV a broad
spectrum PCN + B-lactamace inhibitor for MRSA
227
 Antituberculars
 Ethambutol (Myambutol)
 RARE retrobulbar neuritis & blindness
 GI upset
 INH isoniazid (Nydrazid)
 Peripheral neuritis & rarely hepatotoxicity
 Don’t give for prophylaxis after age 40
because of increase in side effects
 Peripheral neuropathy
 Selegiline (SEL)-like syndrome
 Pyrazinamide
 Hepatotoxicity & hyperuricemia
 (reports of liver failure)
 Rifampin
 Hepatitis, body fluids turn orange/red color
 Streptomycin 228
 Latent TB

 If skin test is positive

 Follow up with chest x-ray

 Use INH for 9 months or rifampin for

4 months for latent TB

229
Antifungal Agents = drug interactions +
liver toxicity
Examples of systemic antifungals
 Itaconazole (Sporanox): inhibitor of cytochrome
3A4 = increased statins, Ca + channel blockers,
some Benzodiazipines, etc.
 Ketoconazole (Nizoral): inhibitor of
cytochrome 2C19 = increased levels of
phenytonin, some Tricyclic Antidepressants,
some Benzodiazipines, etc.
 Fluconazole (Diflucan): inhibitor of
cytochrome 2C9 = increased level of celebrex,
NSAIDs, Warfarin, phenytoin, etc.
230
 Antivirals
 Drugs used to kill viruses
 Inhibit their ability to replicate

 Difficult to kill because they live inside our cells

 Utilize our cells to replicate
 Any drug that kills a virus may kill our cells
 Only work during viral replication
 Mutations & resistance common
 Antimicrobials not effective unless
accompanying secondary bacterial infection

231
 Photo Acknowledgement:
Unless noted otherwise, all photos
and clip art contained in this module
were obtained from the
2003 Microsoft Office Clip Art Gallery.

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