Drug Summary Tables from Katzung J
Table of contents
I. Autonomic drugs
……………………………………………………………………………………………………………………………. 3
A. Cholinoceptoractivating & cholinesteraseinhibiting drugs
B. Cholinoceptor blockers & cholinesterase
regenerators C.Sympathomimetics
D. Adrenoceptor Blockers
II. Cardiovascular drugs
……………………………………………………………………………………………………………………………. 11
A. Drugs used in hypertension
B. Drugs used in the treatment of angina pectoris
C. Drugs used in heart failure
D. Antiarrhythmic drugs
E. Diuretic agents
III. Drugs with important actions on smooth muscles ………………………………………………………………………………………….
24
A. Histamine, serotonin, and ergot alkaloids
B. Vasoactive peptides
C. Prostaglandins and other eicosanoids
D. Nitric oxide, donors and inhibitors
E. Bronchodilators and other drugs used in asthma
IV. Drugs that act in the CNS
…………………………………………………………………………………………………………………………… 32
A. Sedativehypnotic drugs
B. Antiseizure drugs
C. General anesthetics
D. Local anesthetics
E. Skeletal muscle relaxants
2014 Source: Katzung and Trevor’s Pharmacology: Examination and Board Review, 9th ed Page 1
, F. Drugs used in Parkinsonism and other movement disorders
G. Antipsychotic agents and lithium
H. Antidepressants
I. Opioid analgesics and antagonists
V. Drugs with important actions on blood, inflammation and gout …………………………………………………………………… 47
A. Drugs used in coagulation disorders
B. Drugs used in the treatment of hyperlipidemias
C. NSAIDs, acetaminophen, and drugs used in rheumatoid arthritis and gout
VI. Endocrine drugs
……………………………………………………………………………………………………………………………. 54
A. Hypothalamic and pituitary hormones
B. Thyroid and antithyroid drugs
C. Corticosteroids and antagonists
D. Gonadal hormone and inhibitors
E. Pacreatic hormones, antidiabetic agents, and glucagon
F. Drugs that affect bone mineral homeostasis
VII. Chemotherapeutic drugs
…………………………………………………………………………………………………………………………... 67
A. Beta lactam antibiotics and cell wall synthesis inhibitors
B. Chloramphenicol, Tetracyclines, Macrolides, Clindamycin, Streptogramins, & Linezolid
C. Aminoglycosides
D. Sulfonamides, Trimethoprim, & Fluoroquinolones
E. Antimycobacterial Drugs
F. Antifungal Agents
G. Antiviral Chemotherapy & Prophylaxis
H. Miscellaneous Antimicrobial Agents & Urinary Antiseptics
I. Clinical Use of Antimicrobials
J. Antiprotozoal Drugs
K. Antihelminthic Drugs
L. Cancer Chemotherapy
2014 Source: Katzung and Trevor’s Pharmacology: Examination and Board Review, 9th ed Page 2
,VIII. Drugs Used in Gastrointestinal Disorders …………………………………………………………………………………………………..
85
AUTONOMIC DRUGS
Drug Summary Table: CholinoceptorActivating & CholinesteraseInhibiting Drugs
Subclass Mechanism of Action Clinical and Other Pharmacokinetics Toxicities, Interactions
Applications
Directacting, muscarinic
agonists
Bethanechol Activates muscarinic Bladder and bowel atony, Oral, IM activity All parasympathomimetic
(M) receptors; increases for example, after surgery Poor lipid effects: cyclospasm, diarrhea,
IP 3 and DAG or spinal cord injury solubility: does urinary urgency, plus
not enter CNS; vasodilation, reflex
not active in eye tachycardia, and sweating
after topical
application
Duration: 0.3–2 h
Pilocarpine Same as bethanechol; Sjögren’s syndrome Oral, IM activity Similar to bethanechol but may
may also activate EPSP (increases salivation); Good lipid cause vasoconstriction via
via M receptors in was used in glaucoma solubility, topical ganglionic effect
ganglia (causes miosis, activity in eye
cyclospasm)
Muscarine Same as bethanechol Alkaloid found in Low lipid solubility but Mushroom poisoning of fast
mushrooms readily absorbed from gut onset type
Directacting, nicotinic
agonists
Nicotine Activates all nicotinic Smoking cessation (also High lipid Generalized ganglionic
(N) receptors; opens Na used as insecticide) solubility, stimulation: hypertension,
2014 Source: Katzung and Trevor’s Pharmacology: Examination and Board Review, 9th ed Page 3
, K channels in ganglia absorbed by all tachycardia, nausea, vomiting,
and neuromuscular end routes diarrhea
plates For smoking
cessation: usually Major overdose: convulsions,
used as gum or paralysis, coma
transdermal patch
Duration: 4–6 h
Varenicline A partial agonist at Smoking cessation High lipid Hypertension, sweating,
N receptors solubility, oral sensory disturbance, diarrhea,
activity polyuria, menstrual
Duration: ~12 h disturbance
Succinylcholine Nreceptor agonist, NM relaxation Highly polar, used Initial muscle spasms
moderately selective for IV and postoperative pain
neuromuscular (NM) Duration: 5–10 Prolonged action in
end plate min persons with abnormal
butyrylcholinesterase
Indirectacting, alcohol
Edrophonium Inhibitor of Reversal of NM block by Increased parasympathetic
Highly polar; used IV
cholinesterase; amplifier nondepolarizing drugs; effects, especially nausea,
of endogenously diagnosis of myasthenia Duration: 5–10 min vomiting, diarrhea,
released Ach gravis urinary urgency
Indirectacting,
carbamate
Neostigmine Like edrophonium plus Reversal of NM block, Moderately polar Like edrophonium but longer
small direct nicotinic treatment of myasthenia but orally active duration
agonist action Duration: 2–4 h
Pyridostigmine Like edrophonium Treatment of myasthenia Moderately polar Like edrophonium but longer
but orally active duration
Duration: 4–8 h
Physostigmine Like edrophonium Reversal of severe Like edrophonium but longer
Lipid soluble; can be
atropine poisoning (IV); duration plus CNS effects:
occasionally used in acute used topically in the eye seizures
2014 Source: Katzung and Trevor’s Pharmacology: Examination and Board Review, 9th ed Page 4
Table of contents
I. Autonomic drugs
……………………………………………………………………………………………………………………………. 3
A. Cholinoceptoractivating & cholinesteraseinhibiting drugs
B. Cholinoceptor blockers & cholinesterase
regenerators C.Sympathomimetics
D. Adrenoceptor Blockers
II. Cardiovascular drugs
……………………………………………………………………………………………………………………………. 11
A. Drugs used in hypertension
B. Drugs used in the treatment of angina pectoris
C. Drugs used in heart failure
D. Antiarrhythmic drugs
E. Diuretic agents
III. Drugs with important actions on smooth muscles ………………………………………………………………………………………….
24
A. Histamine, serotonin, and ergot alkaloids
B. Vasoactive peptides
C. Prostaglandins and other eicosanoids
D. Nitric oxide, donors and inhibitors
E. Bronchodilators and other drugs used in asthma
IV. Drugs that act in the CNS
…………………………………………………………………………………………………………………………… 32
A. Sedativehypnotic drugs
B. Antiseizure drugs
C. General anesthetics
D. Local anesthetics
E. Skeletal muscle relaxants
2014 Source: Katzung and Trevor’s Pharmacology: Examination and Board Review, 9th ed Page 1
, F. Drugs used in Parkinsonism and other movement disorders
G. Antipsychotic agents and lithium
H. Antidepressants
I. Opioid analgesics and antagonists
V. Drugs with important actions on blood, inflammation and gout …………………………………………………………………… 47
A. Drugs used in coagulation disorders
B. Drugs used in the treatment of hyperlipidemias
C. NSAIDs, acetaminophen, and drugs used in rheumatoid arthritis and gout
VI. Endocrine drugs
……………………………………………………………………………………………………………………………. 54
A. Hypothalamic and pituitary hormones
B. Thyroid and antithyroid drugs
C. Corticosteroids and antagonists
D. Gonadal hormone and inhibitors
E. Pacreatic hormones, antidiabetic agents, and glucagon
F. Drugs that affect bone mineral homeostasis
VII. Chemotherapeutic drugs
…………………………………………………………………………………………………………………………... 67
A. Beta lactam antibiotics and cell wall synthesis inhibitors
B. Chloramphenicol, Tetracyclines, Macrolides, Clindamycin, Streptogramins, & Linezolid
C. Aminoglycosides
D. Sulfonamides, Trimethoprim, & Fluoroquinolones
E. Antimycobacterial Drugs
F. Antifungal Agents
G. Antiviral Chemotherapy & Prophylaxis
H. Miscellaneous Antimicrobial Agents & Urinary Antiseptics
I. Clinical Use of Antimicrobials
J. Antiprotozoal Drugs
K. Antihelminthic Drugs
L. Cancer Chemotherapy
2014 Source: Katzung and Trevor’s Pharmacology: Examination and Board Review, 9th ed Page 2
,VIII. Drugs Used in Gastrointestinal Disorders …………………………………………………………………………………………………..
85
AUTONOMIC DRUGS
Drug Summary Table: CholinoceptorActivating & CholinesteraseInhibiting Drugs
Subclass Mechanism of Action Clinical and Other Pharmacokinetics Toxicities, Interactions
Applications
Directacting, muscarinic
agonists
Bethanechol Activates muscarinic Bladder and bowel atony, Oral, IM activity All parasympathomimetic
(M) receptors; increases for example, after surgery Poor lipid effects: cyclospasm, diarrhea,
IP 3 and DAG or spinal cord injury solubility: does urinary urgency, plus
not enter CNS; vasodilation, reflex
not active in eye tachycardia, and sweating
after topical
application
Duration: 0.3–2 h
Pilocarpine Same as bethanechol; Sjögren’s syndrome Oral, IM activity Similar to bethanechol but may
may also activate EPSP (increases salivation); Good lipid cause vasoconstriction via
via M receptors in was used in glaucoma solubility, topical ganglionic effect
ganglia (causes miosis, activity in eye
cyclospasm)
Muscarine Same as bethanechol Alkaloid found in Low lipid solubility but Mushroom poisoning of fast
mushrooms readily absorbed from gut onset type
Directacting, nicotinic
agonists
Nicotine Activates all nicotinic Smoking cessation (also High lipid Generalized ganglionic
(N) receptors; opens Na used as insecticide) solubility, stimulation: hypertension,
2014 Source: Katzung and Trevor’s Pharmacology: Examination and Board Review, 9th ed Page 3
, K channels in ganglia absorbed by all tachycardia, nausea, vomiting,
and neuromuscular end routes diarrhea
plates For smoking
cessation: usually Major overdose: convulsions,
used as gum or paralysis, coma
transdermal patch
Duration: 4–6 h
Varenicline A partial agonist at Smoking cessation High lipid Hypertension, sweating,
N receptors solubility, oral sensory disturbance, diarrhea,
activity polyuria, menstrual
Duration: ~12 h disturbance
Succinylcholine Nreceptor agonist, NM relaxation Highly polar, used Initial muscle spasms
moderately selective for IV and postoperative pain
neuromuscular (NM) Duration: 5–10 Prolonged action in
end plate min persons with abnormal
butyrylcholinesterase
Indirectacting, alcohol
Edrophonium Inhibitor of Reversal of NM block by Increased parasympathetic
Highly polar; used IV
cholinesterase; amplifier nondepolarizing drugs; effects, especially nausea,
of endogenously diagnosis of myasthenia Duration: 5–10 min vomiting, diarrhea,
released Ach gravis urinary urgency
Indirectacting,
carbamate
Neostigmine Like edrophonium plus Reversal of NM block, Moderately polar Like edrophonium but longer
small direct nicotinic treatment of myasthenia but orally active duration
agonist action Duration: 2–4 h
Pyridostigmine Like edrophonium Treatment of myasthenia Moderately polar Like edrophonium but longer
but orally active duration
Duration: 4–8 h
Physostigmine Like edrophonium Reversal of severe Like edrophonium but longer
Lipid soluble; can be
atropine poisoning (IV); duration plus CNS effects:
occasionally used in acute used topically in the eye seizures
2014 Source: Katzung and Trevor’s Pharmacology: Examination and Board Review, 9th ed Page 4