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Flashcards in Pharmacology 4 Deck (132)
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1
Q

Name 4 therapeutic effects of aspirin.

A

Pain relief

Antipyretic effects

Antirheumatic effects

Anti-inflammatory effects

2
Q

Adverse or toxic effects of aspirin include what 9 things?

A

Occult bleeding from GI tract

Tinnitus

Nausea and vomiting

Acid-base disturbance of metabolic acidosis

Decreased tubular reabsorption of uric acid

Salicylism

Delirium

Hyperventilation

3
Q

Acetaminophen lacks ___ activity. It is hepatotoxic and [causes/does not cause] GI upset

A

Anti-inflammation

Does not cause

4
Q

Which causes more GI irritation, ibuprofen or aspirin?

A

Aspirin

5
Q

True or false… diflunisal (dolobid) has a longer half-life than aspirin, acetaminophen, and ibuprofen

A

True

6
Q

Acetaminophen causes liver toxicity, especially when combined with __ or taken in excess of ___ per day.

A

Alcohol

4grams per day

7
Q

____ is the drug of choice for the feverish child? Why should aspirin be avoided?

A

Acetaminophen

Increased risk of Reye’s syndrome

8
Q

The mechanism of the antipyretic action of salicylates probably results from…

A

Inhibition of prostaglandin synthesis in the CNS affecting hypothalamic temperature regulation

9
Q

True or false.. the antipyretic action of salicylates is explained in part by cutaneous vasoconstriction leading to increased heat loss

A

False.. cutaneous vasoDILATION leading to increased heat loss

10
Q

___ is the locus of action of aspirin’s central antipyretic effect

A

Hypothalamus

11
Q

A patient who has been taking large quantities of aspirin might show increased postoperative bleeding because aspirin inhibits…

A

Synthesis of thromboxane A2 and prevents platelet aggregation

12
Q

True or false… triamcinolone directly inhibits prostaglandin synthetase

A

False… it inhibits phospholipase A2, the enzymatic step that precedes prostaglandin synthesis. Triamcinolone is a corticosteroid, this is how corticosteroids work.

13
Q

True or false… phenylbutazone is an NSAID

A

True

14
Q

Which of the following is NOT produced by excessive doses of acetylsalicylic acid?

Delirium
Tinnitus
Hypothermia 
Hyperventilation 
Metabolic acidosis
A

Hypothermia - it only lowers your temperature if you have a fever. Taking aspirin does not have any affect on body temperature in the non-feverish patient, but high doses can cause all the other effects listed.

15
Q

True or false… acetylsalicylic acid causes methemoglobinemia

A

False

16
Q

True or false… aspirin causes decreased tubular reabsorption of uric acid

A

True

17
Q

True or false… acetaminophen may cause methemoglobinemia at high doses

A

True

18
Q

True or false… acetaminophen is cross-allergic with aspirin.

A

False

19
Q

___ is used in detoxification of opioid addicts

A

Methadone

20
Q

Name 7 pharmacological effects of morphine

A

Respiratory depression

Euphoria

Sedation

Dysphoria

Analgesia

Constipation

Urinary retention

21
Q

What is the mechanism of respiratory depression in an opioid overdose?

A

Loss of sensitivity of the medullary respiratory center to carbon dioxide

22
Q

True or false… narcotic ingestion can lead to bronchiolar constriction and increase in intracranial pressure

A

True

23
Q

Which drugs suppress the cough reflex?

A

Opioids

24
Q

Morphine binds to ___ receptors in the __ to produce analgesia

A

Mu

CNS

25
Q

Morphine causes vomiting by…

A

Stimulation of the medullary chemoreceptors trigger zone

26
Q

Barbiturates and opiates depress respiration primarily by…

A

Rendering the respiratory center in the brain stem less sensitive to changes in CO2

27
Q

The cause of death with opioid intoxication is ___

A

Respiratory depression

28
Q

True or false… pentazocine has both agonistic and antagonistic activities

A

True

29
Q

A heroin-dependent patient should NOT be given nalbuphine for pain because…

A

As a mixed agonist-antagonist, it can elicit withdrawal symptoms

30
Q

True or false… pentazocine is effective only on parenteral administration

A

False.

31
Q

Why is methadone used in detoxification (drug withdrawal) of patients physically dependent on morphine?

A

Withdrawal reactions are less intense and stressful than those of morphine

32
Q

True or false… methadone is a full agonist with analgesic properties, just like morphine

A

True. However, when taken orally, it is not euphoric in addicts, but acts just like morphine to produce tolerance and physical dependence. Withdrawal is less severe than with morphine because methadone has a much longer Half life.

33
Q

___, ___, ___ are competitive muscarinic receptors blockers which sometimes are used to control salivary secretions. ____ specifically, blocks vagal reflexive control of heart rate, resulting in tachycardia

A

Atropine

Scopolamine

Propantheline

Atropine

34
Q

___ and ___ are reversible anticholinesterase that differ in that ___ acts both centrally and peripherally whereas __ only acts peripherally but also has some direct ACh-like activity at the neuromuscular junction, in addition to prolonging the activity of endogenous ACh. They sometimes see use in treating xerostomia

A

Physostigmine
Neostigmine

Physostigmine

Neostigmine

35
Q

___ and ___ are direct acting cholinergic agonists. They may be used for xerostomia

A

Pilocarpine

Methacholine

36
Q

Organophosphates and incentivized irreversibly inhibit ___

A

Cholinesterase

37
Q

___ is an enzyme regenerator used in organophosphate toxicity

A

Pralidoxime

38
Q

___ is a depolarizing neuromuscular junction blocker, subject to rapid inactivation by plasma pseudocholinesterase. It is used to prevent laryngospasm

A

Succinylcholine

39
Q

___ is a non-depolarizing neuromuscular junciton blocker

A

D-tubocurarine

40
Q

__ and ___ are ganglionic blockers that produce orthostatic hypotension

A

Mecamylamine

Hexamethonium

41
Q

Name 6 symptoms of a cholinergic crisis. What do you use to treat it?

A
Bradycardia
Lacrimation
Salivation
Voluntary muscle weakness
Diarrhea
Bronchoconstriction 

Atropine

42
Q

What are 5 symptoms of a scopolamine overdose? What do you use to treat it?

A
Disorientation
Confusion
Hallucinations
Burning dry mouth
Hyperthermia 

Physostigmine

43
Q

Atropine blocks the __ reflexive control of heart rate, resulting in [bradycardia/tachycardia]

A

Vagal

Tachycardia

44
Q

Neostigmine produces its effect by ___

A

Inhibition of acetylcholinesterase activity (similar to physostigmine, however these differe from the insecticides and nerve gases listed below in that they are reversible and can be used clinically; the latter are irreversible)

45
Q

Name two ganglionic nicotinic blocking agents

A

Mecamylamine

Trimethaphan

46
Q

How can neostigmine stimulate denervated skeletal muscle?

A

It is capable of acting directly on the endplate

47
Q

Which drug can be used to prevent laryngospasm?

A

Succinylcholine (it is a nicotinic antagonist - skeletal muscle relaxant)

48
Q

Outline the cholinergic stimulation effects

A

Eye: miosis and reduction of intraocular pressure

CV: bradycardia; vasodilation (but only from injected cholinergic agents, since the muscrinic receptors on the vascular smooth muscle has no neural input)

GI tract: increased spasmodic activity, increased salivation and acid secretion (overdose; nausea, vomiting, diarrhea)

urinary tract: increased uringation

Resipiratory: bronchoconstriction

Glandular: lacrimation, sweating

Skeletal muscle: tremor and ataxia (overdose; muscle weakness, cramps and fasiculations)

49
Q

out line the anticholinergic (antimuscarnic) actions

A

Eye: mydriasis and loss of accommodation and increase of intraocular pressure

CV: increased heart rate (overdose: tachycardia

GI tract: decreased spasmodic activity, decreased salivation and acid secretion (overdose)

Urinary tract: decreased urination

Respiratory: bronchodilator

Glandular: decreased lacrimation, decrease sweating (overdose: hot, dry skin, hyperthermia)

Skeletal muscle: no effects, since they don’t act on nicotinic receptors, only muscarinic

CNS: tertiary amines such as atropine get into the brain and cause restlessness, headache, excitement, hallucinations and delirium

Quaternary amines like methantheline and propantheline only have peripheral actions

50
Q

How does tachycardia result from administration of atropine or scopolamine?

A

Blockade of vagus nerve activity

Atropine and scopolamine are muscarinic cholinergic receptor blockers.

51
Q

All of the following are possible effects of cholinomimetic drugs except…

Mydriasis
Bradycardia 
Increased peristalsis
Stimulation of sweat glands
Increased secretion by bronchial glands
A

Mydriasis

52
Q

True or false.. in addition to anticholinergic effects, atropine overdose causes CNS excitation and tachycardia

A

True

This is atropine isn’t used for sedation. (Scolopamine may be used for sedation because it doesn’t have this effect)

53
Q

True or false physostigmine is an indirect acetylchoniesterase that will function to increase cholinergic action

A

True

54
Q

Succinylcholine is a short-acting neuromuscular junction blocking agent useful for providing a brief paralysis to aid in incubating patients. It is short-acting because…

A

It is subject to inactivation by plasma esterases

55
Q

Receptor blockers (alpha or beta adrenergic drugs such as prazosin or propranolol respectively) act by [competitive/noncompetitive] inhibition of ____ receptors

A

Competitive

Postjuncitonal

56
Q

What is reserpine?

A

Depletes NE by inhibiting its reuptake

57
Q

What is guanethidine?

A

Inhibits the release of catecholamines

58
Q

What is alpha methyldopa?

A

Acts centrally as a false neurotransmitter which gets taken up into storage vesicles and released with NE, thus decreasing sympathetic activity

59
Q

What is clonidine?

A

Stimulates A2 receptors in CNS with a resulting decrease in sympathetic outflow

60
Q

What is “epinephrine reversal”?

A

In the presence of an alpha blocker (usually they give prazosin, but drugs such as chlorpromazine may also be given) epi causes decrease in blood pressure rather than increase because beta mediated vasodilation predominates

61
Q

What is the vagal reflex?

A

Injection of a pressor dose of NE may result in decreased heart rate due to activation of barorecptors which stimulate vagal reflex to reduce heart rate.

62
Q

The vagal reflex is blocked by which drug?

A

Atropine

63
Q

What are the results of alpha-1 receptor stimulation? (3 things)

A

Vasoconstriction

Urinary retention

Mydriasis

64
Q

Name three effects of beta receptor stimulation.

A

Increased heart rate (b1)

Bronchodilation (B2)

Vasodilation (B2)

65
Q

Alpha-1 block results in vaso[dilation/constriction].

A

Vasodilation

66
Q

What happens when beta receptors are blocked?

A

Decreased heart rate (B1)

Bronchoconstriction (B2)

67
Q

Carbidopa is given with levodopa to block ___ activity in the periphery, which in the absence of carbidopa, converts the levodopa to DA in the periophary, decreasing the amount of levodopa that ends up in the brain. ___ is sympathomimetic, and will produce sympathetic stimulation in the periphery. Results in Development of abnormal facial movement, nausea and vomiting, cardiac arrhythmias, and mental disturbances.

A

Dopa decarboxylase

Levodopa

68
Q

Describe the mechanism of action of guanethidine

A

Uncoupling of the action potential from the NE release mechanism

69
Q

___ and ___ are the only centrally acting antihypertensives, reducing sympathetic outflow via alpha-1 agonist action.

A

Methyldopa

Clonidine

70
Q

What is the mechanism of action of reserpine?

A

Stabilize the axon terminal membrane thus preventing release of NE

71
Q

Pretreatment with ___ prevents a response to amphetamines because…

A

Reserpine

Causes depletion of NE from storage sites, thus it cannot be released by amphetamine.

72
Q

What are the effects of alpha 1 agonists?

A

Increased smooth muscle tone leading to VASOCONSTRICTION and INCREASED blood pressure

73
Q

What are the effects of alpha-2 agonists?

A

Can cause hypotension by reducing sympathetic outflow from the CNS

74
Q

What are the affects of B-1 agonists?

A

Increased cardiac rate and force of contraction, thus positive inotropic and chronotropic actions

75
Q

What are the effects of Beta-2 agonists?

A

Dilation of skeletal muscle blood vessels and bronchi or relaxation of bronchiolar smooth muscle

76
Q

Phenolamine is a ___ blocker.

A

Alpha

77
Q

Injection of epi usually causes a rise in blood pressure due to what 3 things?

A

Myocardial stimulation that increases ventricular contraction

An increase in heart rate

Vasoconstriction due to alpha receptor stimulation

78
Q

True or false… NE stimulates alpha and beta 1 receptors more than beta 2

A

True

79
Q

Phenylephrine is a ___ agonist used for ___

A

Alpha-1

Stuffy noses

80
Q

___ is the phenomenon in which two drugs produce opposite effects on a physiologic system but do not act at the same receptor site.

A

Physiologic antagonism

81
Q

_____ reactions to drugs are related to genetic factors and they are the least predictable.

A

Idiosyncratic

82
Q

Two drugs, A and B, have the same mechanism of action. Drug A in a dose of 5mg produces the same magnitude of response as drug B in a dose of 500mg. Drug A is 100x as ___

A

Potent

83
Q

What is the occupational theory of drug-receptor interaction?

A

The magnitude of the drug response is proportional to the number of receptors occupied

An antagonist drug has affinity but no intrinsic activity

The degree of drug action is dependent on the law of mass action

84
Q

What is the mechanism of action of benzodiazepines?

A

Modulate the activity of the inhibitory neurotransmitter, GABA

85
Q

What are 4 advantages of benzodiazepines over barbiturates?

A

Less addiction potential

Less profound CNS depression

Larger therapeutic index

Less respiratory depression

86
Q

IV injection of diazepam can cause irritation such as ____ due to solvent in the benzodiazepine is dissolved in.

A

Thrombophlebitis

Also note that many benzos form active metabolites

87
Q

Thiopental’s action is terminated by…

A

Redistribution of the drug out of the brain. It enters the brain rapidly and exits rapidly. Thus it has a quick onset and short duration of action

88
Q

True or false… barbiturates provide profound analgesia

A

False.. barbs are not analgesic at all

89
Q

How are barbiturate overdoses lethal?

A

Respiratory depression

90
Q

Barbiturates are contraindicated in pateints with ____ because…

A

Intermittent porphyria

Barbs enhance porphyrin synthesis and thus will aggravate the disease.

91
Q

Benzodiazepines exert their main effect on ____

A

Central GABAergic neurons

92
Q

Barbiturates [increase/decrease] secretions

A

Decrease

93
Q

The action of the ultrashort-acting barbiturates is terminated primarily by the process of ___

A

Redistribution

94
Q

Barbiturates are metabolized by the ___, the are classified according to duration of action (thiopental is __acting, phenobarbital is ___acting), and they depress all levels of the CNS

A

Liver

Thiopental

Phenobarbital

95
Q

If diazepam is to be given intravenously, it is recommended that a [small/large] vein be used in order to decrease the risk of ___

A

Large

Thrombophlebitis

96
Q

What is the mechanism of antipsychotic action?

A

Blockade of dopaminergic sites in the brain

97
Q

What are the Two major side effects of antipsychotics?

A

Anticholinergic effects

Extrapyramidal stimulation resulting in tardive dyskinesia

98
Q

2nd generation antipsychotics, like clozapine, block __ and ___ receptors. They treat ___ symptoms. They have [fewer/more] extrapyramidal side effects like tardive dyskinesia.

A

Dopamine
Serotonin (5-HT)

Negative

Fewer

99
Q

What are the main side effects of antidepressants?

A

Anticholinergic or atropine-like side effects

100
Q

___ is the drug of choic for the manic phase of manic depression (bipolar)

A

Lithium

101
Q

True or false… antipsychotic drugs cause emesis (vomiting).

A

False. They are effective ANTIemetics and are often used clinically for this purpose.

102
Q

Antipsychotics [block/stimulate] the dopamine receptor. They also affect the hypothalamic temperature regulation system

A

Block

103
Q

The antipsychotic effects of phenothiazines are the result of ___

A

Blockade of dopaminergic sites in the brain

104
Q

___ is the prototypic phenothiazine, an antipsychotic drug used in the treatment of schizophrenia. Other antipsychotic drugs used for this purpose are __ and ___.

A

Haloperidol

Thioridazine

105
Q

What is an irreversible side-effect resulting from long-term administration of phenothiazines?

A

Tardive dyskinesia

106
Q

Tardive dyskinesia is a neurological side-effect of which drug class?

A

Phenothiazine antipsychotics

107
Q

True or false… Phenothiazine derivatives result in gingival hyperplasia

A

False..

It does result in jaundice, xerostomia, postural hypotension, and symptoms of Parkinsonism

108
Q

Imipramine is a ___. Tranylcyopromine is a ___

A

Tricyclic antidepressant

MAOI

109
Q

What is the major mechanism of action of tricyclic antidepressants?

A

Blockade of the reuptake of amine neurotransmitters released into the synaptic cleft.

110
Q

Tricyclic antidepressants have a prominent side effect that most nearly resembles the usual pharmacological action of ___

A

Atropine

TCAs are strong anticholinergics

111
Q

True or false… corticosteroids or glucocorticoids suppress the immune system in addition to their antiinflammatory action. This can cause latent TB infections to go systemic

A

True

112
Q

Name 8 side effects of corticosteroids/glucocorticoids

A

Gastric ulcers

Immunosuppression

Acute adrenal insufficiency

Osteoporosis

Hyperglycemia

Redistribution of body fat

113
Q

True or false… adrenal corticosteroids cause retention of sodium and fluid. They decrease activity in lymphoid tissue. They can produce a diabetes-like syndrome with high blood levels.

A

True

114
Q

___ is contraindicated in a patient with AIDS, candidiasis, TB, or peptic ulcers.

A

Corticosteroids

115
Q

Glucocorticosteroids are useful as secondary treatment of anaphylaxis because they…

A

Suppress the inflammatory response to cell injury

116
Q

___ are used successfully to treat Addison disease, lupus erythematosus, rheumatoid arthritis, and apthous stomatitis.

A

Adrenal steroids

117
Q

True or false… the onset of anesthesia is inversely proportional to solubility of the anesthetic in the blood.

A

True. The more soluble the agent is in the blood, the more must be given to reach critical tension in the brain

118
Q

The general anesthetic, Halothane, is associated with what adverse side effect?

A

Hepatotoxicity

119
Q

Name the 4 stages of anesthesia

A

Stage 1: analgesia

Stage 2: delirium

Stage 3: surgical anesthesia

Stage 4: medullary paralysis

120
Q

Signs and stages of anesthesia are most likely to be seen with a general anesthetic that has a [slow/fast] rate of induction

A

Slow

121
Q

The behavior of pateints under general anesthesia suggests that the most resistant part of the CNS is the ___

A

Medulla oblongata

122
Q

In general anesthesia, the last part of the CNS to be depressed is the __

A

Medulla (stage 4)

123
Q

H1 antihistamines are useful for treating ____

A

Dermatological manifestations of an allergic response (chlorpheniramine)

124
Q

H1 antihistamines are used preoperatively for ___, ___ properties, and ____ effects.

A

Sedation

Antiemetic

Anticholinergic

125
Q

True or false… antihistamines are used in controlling symptoms of Parkinsonism

A

True (ex. Diphenhydramine)

126
Q

H2 antihistamines such as cimetidine are used to ____

A

Reduce gastric acid secretion (now available OTC for heartburn)

127
Q

What is chlorpheniramine and what is it used for?

A

Antihistamine (H1)

Used for treating dermatological manifestations of an allergic response

128
Q

What is cimetidine and what is it used for?

A

H2 antihistamine. Used to decrease gastric acid secretion

129
Q

Which antihistamine is most commonly used as preoperative medication?

A

Promethazine (used for vertigo)

130
Q

The use of diphenhydramine (Benadryl) in controlling the symptoms of Parkinsonism is based on its ___ effects.

A

Anticholinergic

131
Q

The mechanism of action of H1 antihistamines is ___

A

Competitive antagonism

132
Q

Which drug is used to treat trigeminal neuralgia?

A

Carbamazepine