PHARMA prelim Flashcards

1
Q

Study of drugs and their actions on living organisms

A

Pharmacology

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2
Q

Pharmacology greek origin and meaning

A

Pharmakon - drugs
Logos - science

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3
Q

Chemical substances that have an effect on living organisms

A

Drug

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4
Q

Chemical constitution of the drug

A

Chemical Name

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5
Q

Common name; Name listed in the US Food
and Drug Administration

A

Generic Name

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6
Q

Name given by the manufacturer

A

Brand Name

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7
Q

Identify the source of drugs:
○ Digitalis, Morphine, Codeine

A

Plants

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8
Q

Identify the source of drugs:
insulin, thyroid drugs

A

Animal Products

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9
Q

Identify the source of drugs:
○ aluminum -> antacid
○ Fluoride -> prevent dental cav
○ Gold -> rheumatoid arthritis
○ Iron -> anemia

A

Inorganic Compounds

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10
Q

Identify the Classification of drugs:
● Those given by injection
● Hypnotic Drugs
● Narcotics
● Habit-forming Drugs
● Drugs that are unsafe unless administered under the supervision of
a licensed practitioner
● New drugs that are investigated

A

Prescription drugs

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11
Q

Identify the Classification of drugs:
● Available without prescription
○ Category I = safe and effective
○ Category II = either unsafe or ineffective
○ Category III = insufficient data to classify

A

Over the Counter Drugs

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12
Q

Identify the Classification of drugs:
● Discovered but are not financially viable and not yet adopted by
any drug company
● Treat rare disease

A

Orphan Drugs

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13
Q

Identify the Drug Evaluation:
● Chemicals are tested to determine whether they have effects
● Evaluate adverse effects

A

Preclinical Trials

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14
Q

Identify the Drug Evaluation:
● Healthy volunteers to test drugs

A

Phase I Studies

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15
Q

Identify the Drug Evaluation:
● Try drugs to patients who have the disease
● Performed at various studies

A

Phase II Studies

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16
Q

Identify the Drug Evaluation:
● Use of drug in vast clinical market
● NOTE: After phase III, there would be a continuous evaluation

A

Phase III Studies

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17
Q

Identify the Drug Evaluation:
● Lack therapeutic activity
● Too toxic, teratogenic
● Small safety margin, produce unacceptable side effects
● Have a low benefit to risk ratio
● Not as effective as available drugs

A

Drug Dropped from the study

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18
Q

Identify the Pregnancy Categories:
No risk to fetus in the 1st trimester and later

A

Category A

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19
Q

Identify the Pregnancy Categories:
Animal studies = no risk to fetus

No adequate studies in pregnant women have shown
an adverse effects Little to NO RISK to the fetus in the
1st trimester

A

Category B

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20
Q

Identify the Pregnancy Categories:
Animal studies = no risk to fetus
May be acceptable
No adequate studies on humans

A

Category C

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21
Q

Identify the Pregnancy Categories:
Human fetal risk
Benefit vs. risk
Life threatening situation
Weigh, explain properly through therapeutic
communication, and discuss the benefits and risk for
both the mother and the baby

A

Category D

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22
Q

Identify the Pregnancy Categories:
Human fetal risk proven
Risk on use of pregnant women

A

Category X

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23
Q

Identify the Controlled Substances:
High abuse potential drugs
No accepted medical use
● Ex: Heroin, marijuana, LSD

A

Schedule I (C-I)

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24
Q

Identify the Controlled Substances:
High abuse potential
Accepted medical use
Severe dependence liability
● Ex: Narcotics, barbiturates

A

Schedule II (C-II)

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Identify the Controlled Substances: Less abuse potential Moderate dependents Medically accepted drugs ● Ex: Nonamphetamine stimulants, codeine preparations, paregoric, nonnarcotic drugs
Schedule III (C-III)
26
Identify the Controlled Substances: Less abuse Limited dependence Antianxiety, sedative Medically accepted drugs ● Ex: Phenobarbital (luminal), benzodiazepines
Schedule IV (C-IV)
27
Identify the Controlled Substances: Limited abuse potential Medically accepted drugs ● Ex: Opioid-controlled substances for diarrhea and cough
Schedule V (C-V)
28
Nurses CANNOT prescribe
True
29
COMPREHENSIVE DANGEROUS DRUG ACT OF 2002 ● Practitioner, who shall prescribe any dangerous drug to any person whose physical or physiological condition does not require the use ● Imprisonment ranging from 12 years and 1 day to 20 years and a fine ranging from P100,000.00 to P500,000.00 and the additional penalty of the revocation of his/her license to practice
RA ACT 9165
30
GENERICS ACT OF 1988 ● Generic Name ○ identification of drugs with scientifically and internationally recognized active ingredients ○ promote, encourage and require the use of generic terminology in the importation, manufacture, distribution, marketing, advertising and promotion, prescription and dispensing of drugs ○ ensure the adequate supply of drugs with generic names at the lowest possible cost and endeavor to make them available for free to indigent patients
RA ACT 6675
31
- GENERICS ACT OF 1988 ● Essential Drug List ○ List of drugs prepared by DOH on the basis of health conditions in the Philippines as well as internationally accepted criteria
RA ACT 6675
32
NARCOTIC DRUG ACT ● Registration and imposition of license on all persons who deal with narcotic drugs and the control of the legal traffic in narcotic drugs
RA 953
33
drugs which produces insensibility, stupor, melancholy or dullness of mind, habit forming
Narcotics
34
drugs with opium, cocoa leaf, heroine, morphine, LSD
Prohibited Drugs
35
self-inducing sedatives, secobarbitals, hypnotic drugs
Regulated Drug
36
EXPANDED SENIOR CITIZENS ACT gives privileges to elderly Filipinos 60 years and above. ● Entitled to 20% discount and exempted from VAT ( value added tax) ● For medicines, generic and branded, vitamins and mineral supplements with doctor’s prescription
Republic Act 9994
37
Name the steps of pharmaceutic phase
Tablet - Disintegration - Dissolution
38
Process of drug movement to achieve drug action
Pharmacokinetics
39
Four Processes of pharmacokinetics
○ Absorption ○ Distribution ○ Metabolism ○ Excretion
40
Movement of drug particles from the GI tract to body fluids by PASSIVE, ACTIVE absorption or pinocytosis.
Absorbtion
41
occurs by diffusion
Passive absorption
42
requires carrier, thus energy to transport
Active absorption
43
cells engulfing the drug particles
Pinocytosis
44
■ “Hepatic First Pass” ■ Drug passes to the liver first
Absorption Principles
45
percentage of the drug that reaches the systemic circulation
Bioavailability
46
Process when drug becomes available to body fluids and tissues
Distribution
47
■ Drugs bind to protein; the portion that is bound is INACTIVE, while the portion that is unbound is ACTIVE or FREE drug. ■ two or more highly protein-bound drugs are given at the same time - free drug in the circulation - toxicity protein level - protein binding sites - free drug – drug accumulation/toxicity
Protein-binding Effect
48
■ allows only lipid-soluble drugs ■ Factors that affects Protein Levels: ● Nutrition ● Age ● Liver and Kidney Disease
Blood-brain Barrier
49
● “biotransformation” ● Process by which body inactivates the drug ● GI tract, LIVER
Metabolism
50
The time it takes for one half of the drug concentration to be eliminated
Half-life
51
What is considered a short half life
4-8 hours
52
What is considered a long half-life
24, 36 and longer
53
○ In 12 hours, half of the 50 mg (25mg) would remain. ○ In another 12 hours (24 hours), half of 25mg (12.5mg) remains. ■ After 36 hours = 6.25mg ■ After 48 hours = 3.125mg ■ After 60 hours = 1.56mg ■ After 72 hours = 0.78mg ■ After 84 hours = 0.39mg ■ After 86 hours = 0.195mg ■ After 108 hours = 0.097mg ● IT WOULD TAKE 4 1⁄2 to 5 DAYS TO CLEAR THE DRUG WITH A HALF-LIFE OF 12 HOURS.
54
In excretion this Filters free unbound protein and water soluble drugs; ○ Laboratory results that decipher that kidneys are excreting correctly:
Excretion
55
Study of drug concentration and its effects on the body
Pharmacodynamics
56
Desirable effects
Primary Effect
57
Desirable of undesirable effects
Secondary Effects
58
Time it takes to reach the minimum effective concentration
Onset
59
Drug reaches its highest blood concentration
Peak
60
Time the drug has its pharmacologic effect
Duration
61
Drug works to initiate a response
Agonists
62
Drugs works to block a response
Antagonists
63
Receptor produces a variety of effects on different organs
Nonspecific Drug Effects
64
Affects different receptor sites
Non-selective drug effects
65
Drug action which increases production
Stimulation
66
Drug action which reduces production
Depression
67
Drug providing something lacking
Replacement
68
Static of production or killing
Inhibition or killing of organisms
69
Measures the margin of safety of a drug It is the ratio that measures the effective therapeutic dose and the lethal dose
Therapeutic index
70
Narrow margins of safety
Increased TI (safe)
71
Wide margins of safety
Decreased TI (toxic)
72
when immediate response is desired. After loading dose, a prescribed daily dose is ordered
Large initial dose
73
Response to the drug tolerance to narcotics
Tolerance/ tachyphylaxis
74
physiologic effects not related to desired drug effects
Side effects
75
more severe that side effects = anaphylaxis, cardiovascular collapse
Adverse reactions
76
- toxicity due to overdosing or drug accumulation
Toxic effects
77
- diurnal rhythm of CNS and endocrine, acid-base balance, hydration, electrolyte
Physiologic Factors
78
Identify the Pathological Factor: affect absorption
GI disorders
79
Identify the Pathological Factor: affect distribution
Vascular problem
80
Identify the Pathological Factor: affects metabolism and excretion
Liver and kidney dose
81
Allergies
Immunological Factors
82
Placebo effect, nocebo
Psychological aspects
83
Consider cold/hot weather
Environmental factors
84
Alcohol ingestion, food integration
Cumulative Effects
85
■ Distribution (Aspirin vs methotrexate for protein binding sites) ■ Biotransformation (Warfarin [coumadin] - metabolize quickly with barbiturates, rifampin ■ Excretion (Digoxin vs. quinidine)
Drug-to-drug interactions
86
■ Oral drugs - empty stomach ■ Tetracycline vs. iron and calcium products ■ MAO Inhibitors vs. cheese, wine, organ meat, beer, yogurt, sour cream, bananas ■ Nitrofurantoin (Macrodantin), Metoprolol (Lopressor), Lovastatin (Mevacor) = mealtime
Drug-to-food interactions
87
■ Delteparin (Fragmin) on AST and ALT ■ ↓K, ↓Mg, ↑ Ca levels = digitalis toxicity ■ TDM (Therapeutic Drug Metabolism)
Drug-laboratory test interactions
88
drug form, route of drug administration, multiple drug therapy, drug interactions
Administration
89
- synergistically working
Adjunct Drugs
90
onset, peak, duration, therapeutic range, side effects, adverse reactions
Pharmacodynamics
91
age, weight, present health disorder, other clinical entities, client drug compliance
Clinical Factors
92
■ Development of adverse effects from simple over dosage ■ Example: anticoagulant therapy→ bleeding
Primary Action
93
■ Excessive response to drugs ■ Kidney problems, other underlying problem
Hypersensitivity
94
○ when body forms antibodies to a particular drug inducing a response in the subsequent exposure ○ Hives,rash, difficulty breathing, increased BP
Drug Allergy
95
adverse effects in various tissues, structures, and organs
Drug-Induced Tissue and Organ Damage
96
○ Rashes, Hives ■ Intervention: ● Frequent skin care ● Instruct to avoid rubbing, tight or rough clothing and harsh soaps ● Administer antihistamines as appropriate. ○ Stomatitis ■ Intervention: ● Frequent mouth care. ● DAT (Diet as Tolerated) with small, frequent feeding. ○ Liver Injury ■ Intervention: ● Discontinue the drug. ● Notify the physician. ○ Renal Injury ■ Intervention: ● Discontinue the drug. ● Notify the physician. ○ Pancytopenia ■ Condition in which the person’s body has too few RBCs, WBCs and platelets. ■ Intervention: ● Discontinue the drug. ● Notify the physician.
97
Two drugs with similar action
Additive Drug Effect
98
Two or more drugs, one drug potentiates the other
Synergistic Drug Effect or Potentiation
99
Two drugs have opposite effects → each drug cancel the effect of the other
Antagonistic Drug Effect
100
● aa = of each ● ac = before meals ● ad lib = as much as desired ● bid = 2x a day ● caps = capsules ● hs = at bedtime ● od = right eye ● os = left eye ● ou = both eyes ● pc = after meals ● prn = as needed ● q= every ● qd = once daily; OD ● qid = 4x a day ● ss = 1⁄2 ● stat = at once ● tid = 3x a daY ● ut dict. = as directed
101
10 R's
102
Identify the categories of drug order: Dr.’s order upon admission, continual unless ordered
Standing
103
Identify the categories of drug order: Demerol 100 mg IM to be given 10minutes prior to surgery
One-time
104
Identify the categories of drug order: ○ Paracetamol 500 mg q4h as needed for headache ○ Medication as needed
PRN
105
Identify the categories of drug order: To be given now
Stat
106
Oral meds are NOT given to clients who are vomiting, lack a gag reflex, or who are comatose. ○ Do not mix in infant formula. ○ Do not mix with a large amount of food or beverage. ○ Enteric-coated and timed-release capsules must be swallowed whole to be effective.
Tablets and capsules
107
Provide gradual but continuous release of the drug
Times-release capsule
108
Flat disks; flavored base
Lozenges
109
Clear liquids dissolved in alcohol and water
Elixirs
110
Water-in-oil; oil-in-water; gelatin
Emulsion
111
Liquid that contain solid, insoluble drug particles, has granules -- needs to be shaken
Suspensions
112
Dissolved in sugar
Syrups
113
○ Read labels → dilute? Shake? ○ Refrigerate
Liquids
114
○ Do not cut patches. ○ Remove patches with metallic components prior to MRI. ○ Remove the old patch prior to applying the new one.
Transdermal
115
○ Do not “double dip.”
Topical
116
○ Gently pull down the skin below the eye to expose the conjunctival sac.
Administration of Eye drops
117
○ Squeeze a 1⁄4-inch-wide strip of ointment onto the conjunctival sac. (inner to outer canthus)
Administration of Eye Ointment
118
○ Straighten the external ear canal by: ■ pulling down and back on the auricle in children or ■ pulling up and back on the auricle in adult
Administration of Ear Drops
119
○ Vaginal ○ Rectum
Inserting a suppository
120
Identify the administration of parenteral Medications: Skin testing
Intradermal
121
Identify the administration of parenteral Medications: thighs
subcutaneous
122
Identify the administration of parenteral Medications: upper outer quadrant of buttocks, deltoid
Intramuscular
123
Identify the administration of parenteral Medications: fastest
intravenous injection
124
U , U - Unit IU - International Unit Q.D - Daily QOD - Every other day TRAILING ZERO - Delete e.g. [1.0 mg = 1 mg] LACK OF LEADING ZERO - Insert e.g. [.2 mg = 0.2 mg] MS MSO4 - Morphine Sulfate MGSO4 - Magnesium Sulfate
125
○ Round off IV drop rates to whole numbers ○ Round off medications in the nearest tenths
125
AD - Right ear AS - Left ear AU - Both ears OD - Right eye OS - Left eye OU - Both eyes BT - Bed time cc - mL for mililiters HS - bedtime qhs - nightly Q6 - 6pm every night/daily qid - four times a day qn - nightly X 3d - for 3 days SC, SW, subQ - Subcutaneously ss - one half SSI - Sliding scale (insulin) ug - Mcg > - greaten than < - less than + - and plus @ - at
126
○ 1 g = 1000 mg ○ 1000 g = 1 kg ○ .001 milligram = 1 microgram (mcg) ○ 1mg = 1000mcg ○ 1L = 1000ml ○ 1 ounce = 480 grains (gr) ○ 1 quart = 2 pints (pt) ○ 3 teaspoons (tsp) = 1 tablespoon (tbsp) ○ 2 tablespoons (tbsp) = 1 ounce (oz)
127
○ Temperature ■ C = (F - 32) x 5/9 ■ F = (C x 9/5) + 32 ○ Weight ■ 1 kg = 2.2 pound (lb)
128
● Prescribed = desired (D) ● Have on hand = stock (S) ● Drug form = quantity (Q)
x =D/S × Q
129
Iv fluid calculation
volume/ hour x df/60
130
infusion time formula
x= v/ ml/hr
131
drops per minute formula
x = v*df/ t
132
10 gtt per mL 15 gtt per mL 20 gtt per mL
Macrodrop
133
60 gtt per mL
Microdrop
134
Tubing set with needle
Micro
135
Tubing set without needle
Macro
136
with mesh/strainer
BT set (Blood Transfusion Set)
137
Formula for Intermittent IV Infusion
gtt/min to administer = Amount of solution x gtt/ml (IV set)/ Minutes to administer
138
Where should you measure volume of medication?
Proximal end of plunger
139
In 100-unit insulin syringes, each small black line equals how many units
2 units
140
In 30 and 50-unit insulin syringes, each small black line equals how many units
1 unit
141
What is Fried's Rule?
Age < 1 Child's Dose = Infant's age in months/ 150 months x average adult dose
142
What is Young's Rule
Age 1-12 years Child's Dose = Child's age (in years)/ child's age (in years) + 12 x average adult dose
143
What is Clark's Rule
Using body weight in pounds Age 1-12 years Child's Dose = weight of child (in pounds)/ 150 pounds x average adult dose
144
Surface Area Calculation
Child's Dose = surface area in square meters/1.73 x average adult dose
145
What is the most effective administration of drug for infants
Topical and water soluble drugs are absorbed easily
146
What is a difficult absorption for older adults
Transdermal absorption
147
Infant ● Premature infant -↓ gastric emptying time →↑ toxicity ● Absence of enzyme for hydrolysis →prevent to absorb chloramphenicol ● ↑ total body content = ↑ volume of distribution for water-soluble drugs ● ↓ protein- ↓ binding
148
Older adult ● ↓ cardiac output →tissue perfusion → ↓ transdermal drug absorption ● ↑ gastric pH ● Drugs destroyed by gastric acid are readily absorbed and ↑ in concentration ○ Ampicillin, penicillin ● Drugs dependent on gastric acid are poorly absorbed ○ Aspirin, Phenobarbital ● ↓ gastric emptying time → ↑ toxicity ● Liver impairment = ↓ drug metabolism
149
Study of drugs that alter processes controlled by the nervous system
Neuropharmacology
150
Conducting an action potential down the axon of the neuron
Axonal Conduction
151
Process by which information is carried across the gap between neuron and postsynaptic cell
Synaptic Transmission
152
21 compounds that serve as neurotransmitters Used for psychiatric disorders, suppression of seizures, relief of pain, production of anesthesia
CNS drugs
153
Identify the CNS Drug: Dopamine Epinephrine Serotonin
Monoamine
154
Identify the CNS Drug: Aspartate GABA Glutamate Glycine
Amino Acid
155
Identify the CNS Drug: Adenosine Adenosine monophosphate Adenosine triphosphate
Purine
156
Identify the CNS Drug: Dynorphins Endorphins Enkephalins
Opioid Peptides
157
Identify the CNS Drug: Neurotensin Oxytocin Somatostatin Substance P Vasopressin
Non Opioid Peptides
158
Identify the CNS Drug: Acetylcholine Histamine GABA
Others
159
● Impedes the entry of drugs into the brain ● Passage is limited to lipid-soluble agents or via specific transport systems ● CHILDREN are much more sensitive to CNS drugs than adults
Blood Brain Barrier
160
Antipsychotic and antidepressants
Increased therapeutic effects
161
phenobarbital, antiseizure drug that produces sedation
Decreased side effects
162
Decreased response occurring in the course of prolonged drug use
State in which abrupt discontinuation of drug use will precipitate a withdrawal syndrome
163
Dysregulation of the transmitters serotonin, norepinephrine, dopamine Characteristics: inattentiveness, inability to concentrate, restlessness, hyperactivity, inability to complete tasks and impulsivity
ADHD Attention Deficit Hyperactivity Disorder
164
○ Characterized by falling asleep during normal waking activities [driving/ talking] ○ Unable to move and may collapse
Narcolepsy
165
■ Given to increase child’s attention span and cognitive performance ■ Used to treat narcolepsy
Methylphenidate
166
■ Treatment of narcolepsy
Modafinil
167
■ Stimulate respiration
Analeptics: Xanthine
168
■ Treatment of respiratory depression caused by drug overdose and COPD ■ Never give more than 3 liters per minute because respiratory drive will be gone
Doxapram
169
● Slowly progressive neurodegenerative disorder characterized by tremor, rigidity, postural instability and slowed movement ● Affects the extrapyramidal system which influences movement
Parkinson's Disease
170
Directly/indirectly cause activation of dopamine receptors
Dopaminergic drugs
171
drugs that block receptors for ACh
Anticholinergic Agents
172
Converted to Dopamine and activates dopamine receptors First-line drug/ supplement to dopamine agonist
Dopamine Replacement Levodopa Levodopa/Carbidopa
173
Directly activates DA receptors First line drugs
Dopamine Agonists Pramipexole Ropinirole Bromocriptine
174
Inhibits breakdown of levodopa Adjunct to levodopa
COMT Inhibitors Entacapone Tolcapone
175
Anti-viral but promotes release of dopamine 2nd or 3rd line drug
Dopamine Releaser Amantadine
176
Inhibits breakdown of dopamine For newly diagnosed patients
MAO-B inhibitors Selegiline Rasagiline
177
Levodopa + Maoi = Hypertensive crisis
Tyramine Reaction
178
Drug interactions with Dopaminergic Drugs
● Reduced when taking pyridoxine [VIT B6], phenytoin, benzodiazepines, reserpine and papaverine ● Use with MAOI increases the risk of hypertensive crisis ● Use with antipsychotic reduces the effectiveness of levodopa ● Amantadine may increase anticholinergic adverse effects
179
Identify the Dopaminergic Drugs according to its adverse effects: N&v Orthostatic hypotension Anorexia Neuroleptic malignant syndrome Arrhythmias Confusion
Levodopa
180
Identify the Dopaminergic Drugs according to its adverse effects: Orthostatic hypotension Constipation
Amantadine
181
Identify the Dopaminergic Drugs according to its adverse effects: Orthostatic hypotension Ventricular tachycardia Bradycardia Worsening angina
Bromocriptine
182
Identify the Dopaminergic Drugs according to its adverse effects: Headache Insomnia Dizziness Nausea Arrhythmia
Seleglline
183
Identify the Dopaminergic Drugs according to its adverse effects: Orthostatic hypotension Dizziness Confusion Insomnia
Ropinirole
184
Group of disorders characterized by excessive excitability of neurons in the CNS
Epilepsy
185
General term that applies to all types of epileptic events
Seizure
186
Excitation undergoes limited spread from the focus to adjacent cortical areas
Partial seizure
187
Excitation spreads widely throughout both hemispheres of the brain
Generalized Seizures
188
Abnormal motor phenomenon
Convulsion
189
○ Carbamazepine ○ Gabapentin ○ Lamotrigine ○ Tiagabine ○ Topiramate
Partial Focal Seizures
190
○ Succinimides ■ Ethosuximide ■ Methsuximide ■ Phensuximide ○ Valproic Acid ○ Zonisamide
Absent Seizures
191
○ Suppression of Sodium Influx ■ Prevent electrical activity lessens the excitability ○ Suppression of Calcium Influx ○ Antagonism of Glutamate ■ Excitatory neurotransmitter ○ Potentiation of GABA ■ Inhibitory neurotransmitters
Anti-Epileptic Drugs Mechanism
192
A Hydantoin ○ most commonly prescribed anticonvulsant drug ○ Stabilize nerve cells to keep them from getting overexcited by increasing efflux or decreasing influx of sodium ions
Phenytoin
193
A Barbiturate ○ Effective against partial seizures and generalized tonic-clonic seizures but not absence seizures ○ Suppresses seizures by potentiating the effects of GABA ○ Can be used as daytime sedative “sleeping pills” ○ Able to suppress seizures without causing generalized CNS depression
Phenobarbital
194
An iminostilebenes ○ Cornerstone of epilepsy therapy ○ Active against partial seizures and tonic-clonic seizures but not absence seizures ○ Suppresses neuronal discharge by delaying recovery of sodium channels ○ Has fewer side effects than phenytoin and phenobarbital ○ Rashes, hives and Steven-Johnson Syndrome [fatal inflammatory disease] can occur as adverse reactions ○ Do not drink grapefruit juice as it can increase levels of this drug
Carbamazepine
195
A Benzodiazepine ○ is restricted to acute treatment of status epilepticus ○ Not recommended for long-term use due to high potential for addiction
Diazepam
196
A Benzodiazepine ○ DOC for acute management of status epilepticus
IV Lorazepam
197
A Benzodiazepine Treatment for absence, atypical absence seizures
Clonazepam
198
Valproate, Valproic Acid, Divalproex ● Mechanism of Action ○ Suppression of neuronal firing though ■ Blocking sodium channels ■ Blocking calcium influx ■ Augment inhibitory influence of GABA ● Indications ○ All partial and generalized seizures ○ Bipolar disorder ○ Migraine
CARBOXYLIC ACID DERIVATIVES
199
Bind to a carrier protein and act at a receptor resulting in increased GABA in the brain
GABAPENTIN
200
Defined as involuntary contraction of a muscle or muscle group ■ Often painful and decreases level of functioning
Muscle Spasm
201
For treatment of acute muscle spasms caused by anxiety, pain and trauma ○ Treat spacity from conditions as MS and Cerebral Palsy ■ Carisoprodol ■ Chlorphenesin ■ Metaxalone ■ Tizanidine
Centrally Acting Agents
202
○ Most effective for spasticity of cerebral origin [i.e. cerebral palsy, MS, spinal cord injury, stroke] ○ Used for treatment of malignant hyperthermia [complication of anesthesia causing muscle rigidity and high fever]
Dantrolene Sodium
203
○ Mimics inhibitory actions of GABA in the CNS ○ Produces less sedation and less peripheral muscle weakness than dantrolene ○ DOC for spasticity ○ Indicated for paraplegic/ quadriplegic patients with spinal cord lesions ○ Most common adverse effect is transient drowsiness
Baclofen
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Relax skeletal muscles by disrupting the transmission of nerve impulses at the motor end plate
NEUROMUSCULAR BLOCKING DRUGS
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● Competitive/ stabilizing drugs ● Compete with ACh to prevent muscle from contracting ○ Atracurium ○ Cisatracurium ○ Doxacurium ○ Mivacurium ○ Pancuronium ○ Rocuronium
NON DEPOLARIZING BLOCKING DRUGS
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○ Use for: ■ Ease of passage of an endotracheal tube ■ Decrease the amount of anesthetic required during surgery ■ Facilitate realigning broken bone and dislocated joints ■ Prevent muscle injury during ECT
Non Depolarizing Agents
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A DEPOLARIZING BLOCKING DRUGS acts like acetylcholine but not inactivated by ACHe ○ DOC for short procedures [less than 3 minutes] and for orthopedic manipulations
Succinylcholine
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Occurs when clients abruptly withdraw from a substance to which they are physically dependent.
Abstinence syndrome
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Identify the Abstinence maintenance: PO, daily, aversion therapy Should not be used concurrently with alcohol
Disulfiram
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Identify the Abstinence maintenance: Opioid antagonist that suppresses craving and pleasurable effects of alcohol
Naltrexone
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Identify the Abstinence maintenance: Decreases unpleasant effects resulting from abstinence (anxiety/ restlessness)
Acamprosate
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Characteristic withdrawal syndrome occurs within 1 hr to several days after cessation of substance use.
Opioid Addiction
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Identify the Opioid withdrawal support: PO, opioid agonist that replaces opioids, prevents abstinence syndrome Part of the 12 step self help program
Methadone
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Identify the Opioid withdrawal support: ● Aids in withdrawal effects related to autonomic hyperactivity (diarrhea, nausea, vomiting)
CLONIDINE (CATAPRES)
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Identify the Opioid withdrawal support: ● Used for detoxification and maintenance, decreases craving, administered SL, IM, IV
BUPRENORPHINE (SUBUTEX)
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The Nervous system compromises of what?
Central and Peripheral
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The cns compromises of what?
Brain and spinal cord
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Peripheral nervous system is compromised of what
Afferent/sensory Efferent/motor: Autonomic nervous system: Sympathetic/adrenergic Parasympathetic/cholinergic Somatic nervous system
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Neurons
Afferent(Sensory) and Efferent (Motor)
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Sends impulses to the CNS
Afferent(Sensory)
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Receives impulses, transmits through the spinal cord to effector organ cells
Efferent (Motor)
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Involuntary Controls and regulates the heart, GI, respiratory system, bladder, eyes and glands
Autonomic ns/ visceral system
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● Voluntary ● Innervates the skeletal muscles
Somatic NS
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○ (1) Synthesis of your neurotransmitter ○ (2) Storage of transmitter in the vesicles ○ (3) Release neurotransmitter because of the response of the action potential ○ (4) Action at the receptor ○ (5) Termination of the synaptic transmission
Synaptic Transmission
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What is the location of the Sympathetic nervous system
Location: thoracolumbar (thoracic and lumbar area)
226
This is also known as the flight or fight response and is the physiological response to non-immediate stresses
Sympathetic nervous system
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What is the terminal neurotransmitter of the Sympathetic nervous system
Norepinephrine
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What is the receptor organ cells of the Sympathetic nervous system
Alpha, beta
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What is the location of the parasympathetic nervous system?
Craniosacral
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Known as the rest and digest response
parasympathetic nervous system
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What is the terminal neurotransmitter of the parasympathetic nervous system
Acetylcholine
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What is the receptor organ cells of the parasympathetic nervous system
Nicotinic, muscarinic
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Dilates pupil, dilates bronchioles, increases heart rate, constricts blood vessels, relaxes smooth muscles of the GI, relaxes uterine muscles
Sympa
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Constricts pupils, constricts bronchioles, increase secretions, decreases heart rate, dilates blood vessels, increases peristalsis, Increases salivation
Parasympa
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○ Drugs act through receptors by binding to the receptors to initiate a response or prevent a response. ○ It is similar to the fit of the right key in a lock.
Receptor Theory
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drugs that produces a response
Agonist
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drugs that blocks a response
Antagonist
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Stimulate the SNS Sympathomimetic
Adrenergic Agonist
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Inhibit the SNS Sympatholytic
Adrenergic antagonist
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Stimulate the PNS Parasympathomimetic
Cholinergic agonist
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Inhibit the PNS Parasympatholytic
Cholinergic Antagonist
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When Autonomic drugs are given, the goal is not to treat an autonomic disorder, it is to correct disorders of target organs through autonomic nerves
Pharmacologic effect
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Blood vessels, vasoconstriction, increased blood pressure, increased contractibility of the heart, eye, mydriasis, bladder relaxation, prostate contraction
Alpha 1 Receptor
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Blood vessels decreased blood pressure, smooth muscle decreased gastrointestinal tone and motility
Alpha 2 receptor
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Heart increased contraction and heart rate, kidney increased renin secretion increased angiotensin increased blood pressure
Beta 1 receptor
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Smooth muscle decreased gastrointestinal tone and mobility, lungs bronchodilation, uterus relaxation, liver activation of glycogenolysis and increased blood sugar
Beta 2 receptor
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stimulate adrenergic receptors Adrenergic agonist
Sympathomimetics
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Drugs that stimulate the sympathetic nervous system. ● Mimics sympathetic neurotransmitters norepinephrine and epinephrine (adrenaline). Also termed adrenergic agonists or adrenergics.
Adrenergic agonist
249
directly stimulates the adrenergic receptor.
Direct-Acting Sympathomimetic
250
stimulates the release of norepinephrine from terminal nerve endings.
Indirect-Acting Sympathomimetic
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acts as both direct and indirect acting ○ Ex. pseudoephedrine
Mixed-Acting Sympathomimetic
252
Has a catechol ring and amines
Catecholamines
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influences one type of receptor
Selective
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influences all receptors
Non-selective
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Treats Hypotension, nasal congestion, dilation of pupils
Alpha 1
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Treats Hypertension
Alpha 2
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Heart failure, cardiac arrest, shock
Beta 1
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Asthma, premature labors of contraction
Beta 2
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● Therapeutic class:: Vasopressor ● Pharmacologic class: Adrenergic ● Indications: anaphylaxis, asthma, cardiac stimulation, induction and maintenance of mydriasis during intraocular surgery ● No oral administration ● Antidote: phentolamine Mesylate (Regitine) for extravasation of norepinephrine and dopamine.
Epinephrine
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Blocks alpha and beta receptor blocker ○ Direct blocking by occupying receptors ○ Indirect blocking by inhibiting release of neurotransmitters
Adrenergic blockers
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○ Vasodilation: hypertension and PVDs ○ Reduces contraction of smooth muscle in bladder and prostate
Alpha blockers
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A decrease of 20 mm Hg or more in SBP, a decrease of 10 mm Hg or more in DBP, and/or ● An increase in the HR of 20 beats/minute or more from supine to standing indicates
Orthostatic hypotension
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● Decrease heart rate ● Decreases blood pressure ● Useful for treating mild to moderate hypertension, angina pectoris and myocardial infarction
Beta blockers
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● Therapeutic class: Anti-hypertensive ● Pharmacologic class: Alpha Blocker ● Indication: mild to moderate hypertension
Prazosin
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○ 5 receptors, stimulate smooth muscle and slows HR ○ M1 (GU) and M3 (lungs, glands) – may increase calcium activity ○ M2 (heart) – may increase potassium and decrease heart rate
Muscarinic
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○ 2 receptors, affect skeletal muscles ○ Nm – muscle contraction ○ Nn – transmission of cholinergic signals
Nicotinic
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is made from choline and acetyl CoA
Acetylcholine (ACh)
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(2) In the synaptic cleft ACh is rapidly broken down by the enzyme
acetylcholinesterase
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Mimic the parasympathetic neurotransmitter acetylcholine
Cholinergic agonists
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Non-specific cholinergic effect, decreases CO, HR, BP, increase GI activity
Acetylcholine
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Not as susceptible to AChE, used locally to constrict pupil and decrease IOP
Carbachol
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Constricts pupil, decrease IOP for acute glaucoma
Pilocarpine
273
Increase muscle tone in bladder ang GIT
Bethanechol
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● Therapeutic class: Urinary Stimulants ● Pharmacologic class: Cholinergic Agonists ● Indications: acute post-operative and postpartum nonobstructive urine retention, neurogenic atony of urinary bladder with urine retention.
Bethanechol
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● Famous for military use as nerve gases ● Clinical use: Echothiophate – treatment of open glaucoma
Indirect acting reversible
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Adverse reactions ● D - Diarrhea ● U - Urination ● M – Miosis and Muscle Weakness ● B - Bronchorrhea ● B - Bradycardia ● E - Emesis ● L - Lacrimation ● S – Salivation/ Sweating
277
● Famous for milit ● Caused by overdose of cholinergic agonists
CHOLINERGIC CRISIS
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Also known as Cholinergic Blockers
Anticholinergic agents
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● Therapeutic Class: Anti-arrhythmics ● Pharmacological Class: Anticholinergic belladonna alkaloids ● Indications: bradycardia, anti-cholinesterase poisoning, preoperatively to diminish secretions and block cardiac vagal reflexes, antimuscarinic
Atropine
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Adverse effects ● A - Agitation ● B - Blurred vision ● C - Constipation, Confusion ● D - Dry mouth ● S - Stasis of urine and Sweating
281
-ganglionic blocker ○ Stimulate and block cholinergic function ○ Increase production of neurotransmitters ○ Increase BP, HR, but may also decrease BP- non-selective effect ○ CNS Stimulation - causes addiction ○ Not useful in clinical practice
Nicotine
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○ Binds to ACh receptors but do not induce ion channel opening ○ Facilitates mechanical ventilator and tracheal intubation ○ Given as IV as it is not absorbed in the GI ○ Rapid effect in less than 2 mins, will paralyze small muscles ○ Includes: ○ Cisatracurium, Pancuronium - 90 mins of MSOF ○ Rocuronium, Vecuronium - 40 mins
Non-depolarizing agents
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Succinylcholine ■ Causes sodium channels to open for prolonged depolarization ■ PHASE I block ■ PHASE II block ■ For rapid sequence tracheal intubation ■ Facilitates ECT ■ Duration: 1-10 mins
Depolarizing agents
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Drug interactions
Sympathomimetic - Parasympathomimetic Sympatholytic - Parasympatholytic