2006 英护本科药理学双语教学作业
Translation for English Nursing Department
承德医学院药理教研室
Department of Pharmacology
Chengde Medical College
June 2008
Editor
Wang Rui-Ting
Associate professor
Authors
Hao
Tong
Shang
Wang
Mei
Li
Zuo
Guan
Xi-Jun
Ji-Ming
Ya-Zhen
Rui--Ting
Ai-Min
Bao-Qun
Yan-Zhen
Li-Hua
郝希俊
佟继铭
商亚珍
王瑞婷
梅爱敏
李宝群
左彦珍
关丽华
Professor
Professor
Professor
Associate professor
Associate professor
Lecturer
Assistant
Lecturer
CONCENTS
Chapter 1 Introduction …………………………………………….. 1
Chapter 2 Pharmacodynamics …………………………………… 2
Chapter 3 Pharmacokinetics ……………………………………... 3
Chapter 4 Autonomic Pharmacology ………………………………..4
Chapter 5 Cholinoceptor-activating and AchE inhibitor ……….….5
Chapter 6 Organophosphates Anticholinesterase Intoxication ……6
Chapter 7 Anticholinergic Drugs (M antagonist) ……...…………7
Chapter 8 Adrenergic Drugs …………………………………………8
Chapter 9 Adrenoceptor Blocking Drugs …………………..….…..10
Chapter 10 Sedative-Hypnotics ………………………..…………….11
Chapter 11 Antiepileptic Drugs ……………..……………………….12
Chapter 12 Antipsychotic Drugs …………………..………………...13
Chapter 13 Analgesics ………………………………………………...15
Chapter 14 Antipyretic-Analgesia and Anti-inflammatory……...…16
Chapter 15 Renin- Angiotensin System …………….…………….…17
Chapter 16 Anti- Arrhythmia Agents …………………………….....18
Chapter 17 Diuretics and Osmotic Diuretics ………………….……19
Chapter 18 Anti-hypertensive Drugs ……………………..…………20
Chapter 19 Drugs for Congestive Heart Failure ……………………21
Chapter 20 Anti-Angina Pectoris Drugs……………..….………..…22
Chapter 21 Drugs Acting on the Blood and Blood Forming Organ 23
Chapter 22 Histamine-Receptor Antagonist……………….……..…24
Chapter 23 Drugs Acting on Respiratory System………………..…25
Chapter 24 Drugs Acting on Digestive System……………..……..…26
Chapter 25 Adrenocortical Hormones……………………………….27
Chapter 26 Agents Affecting the Thyroid Gland………….….…28
Chapter 27 Antidiabetic drugs……………..……………….……...…29
Chapter 28 Antimicrobial Agents…………………………...30
Chapter 29 Beta-lactam antibiotics……………………...…31
Chapter 1 General Principles of Pharmacology- Introduction
1 Pharmacology deals with the chemical and physical properties, action, mechanism
of action, biotransformation , side effects, clinical uses and contraindications of
drugs.
2 Pharmacodynamics is the study of the biochemical and physiological effects of
drugs and their mechanism of action.
3 Pharmacokinetics deals with the changes of drug concentration in the human body
following administration.
4 Drugs are substances used for the purposes of prevention, diagnosis and treatment
of disease.
5 The basic medical knowledge, such as physiology, biochemistry, pathology,
pathophysiology, microbiology, immunology and molecular biology are applied to
elucidate the mechanisms of drugs’ action , and to establish the theoretical basis of
using drugs rationally in clinic.
Pharmacology [] 药理学
biotransformation [] 生物转化
Pharmacodynamics [] 药效学
Pharmacokinetics [] 药代学
Physiology [] 生理学 pathology []
病理学
Elucidate [].阐明
1
Chapter 2 Pharmacodynamics
1 Treatment can be classified into etiological and symptomatic treatment according to
therapeutic effect.
2 Adverse effect includes side effect, toxic effect, residual effect, withdrawal reaction,
allergic reaction, idiocyncrasy.
3 pharmacological effect can be classified into graded response and quantal response
according to effect property.
4 efficacy: the maximum effect of a drugs, it is related to intrinsic activity. Intrinsic
activity is the ability of a drug to produce an effect.
5 potency: refers to the different doses of two drugs that are needed to produce the
same degree of effect. It is related to affinity. Affinity is the tendency of a drug to
combine with the receptor.
6.ED50:the dose at which 50% of the individuals exhibit the specified quantal effect.
7 LD50:the dose at which
50% of the animal exhibit death. Therapeutic
index(TI)=LD50/ED50
8 Agonist: is a drug that has high affinity to receptor and high intrinsic activity,
produces a pharmacological effect when it combines with receptor.
9 An antagonist binds to the receptor to inhibit the action of an agonist, but initiate no
effect themselves. The inhibition can be overcome by increasing the concentration
of the agonist, ultimately achieving the same maximal effect.
10 receptor can be classified into four types: G protein-coupled receptor, ligand-gated
ion channel, tyrosine-protein kinase receptor, intracellular receptor.
11 Affinity: the tendency of a drug to form a combination with the receptors.
12 intrinsic activity:its inherent ability to produce an effect.
13 competitive antagonist: competitive antagonists compete with agonists in a
reversible fashion for the same receptor site . When the antagonist is present, the
log dose-response curve is shifted to the right but the maximal response of the
agonist is unchangeble when increasing concentration of a agonist enoughly.
etiological [] 病 因 的
[]
adverse [] 不利的
efficacy
效能
residual
[] 残 留 的
[] 停药
intrinsic
[] 内 在 的
symptomatic
[]
withdrawal
potency
[`] 效价强度
affinity
[] 亲和力
激动剂
antagonist [] 拮抗剂
酪氨酸
allergic [] 过敏的
的
2
agonist
tyrosine
reversible
[]
[]
[l] 可逆
Chapter 3 Pharmacokinetics
1 Pathways that drugs transporting across membrane include passive diffusion, active
transport, carrier-mediated facilitated diffusion, endocytosis .
2 intracorporeal process of drug includes absorption, distribution,
metabolism,excretion. Absorption is the process that drug enters blood from the
administration site.
3 first- pass elimination: following absorption from the gastrointestinal tract, drugs
pass initially through the hepatic circulation. Some drugs are metabolized so
extensively in the gut wall or liver before they reach the systemic circulation.
4 bioavailability: it is defined as the fraction of unchanged drug reaching the systemic
circulation following administration by any route, it is related to the area under the
plasma concentration-time curve.
5 drug metabolism involves two kinds of biochemical reactions known as phase Ⅰ
and phase Ⅱ reactions. Phase Ⅰ reaction consists of oxidation, reduction or
hydrolysis. Phase Ⅱ reaction involves conjugation, acetylation and methylation.
6 enzyme inducer and enzyme inhibitor
7 first order kinetics: constant fraction of drug is eliminated per unit time.
Zero order kinetics: same quantity of drug is eliminated per unit time.
8 half life: the time taken for the concentration of drug to fall to half of the initial
value.
9 Apparent volume of distribution: a hypothetical volume of body fluid that would be
required to dissolve the total amount of drug at the same concentration as that found
in the blood.
10 steady state: may be defined as a time of no net change in the amount of drug when
rate of input equals rate of output.
11 clearance :is defined as the volume of plasma which would have to lose all the
drug it contains per unit time.
endocytosis
[]
[]体内的
intracorporeal
oxidation
[] 氧化
reduction
还原
hydrolysis
[] 水 解
[] 结合
acetylation
[] 乙 酰 化
[] 甲基化
hepatic [] 肝的
[]
conjugation
methylation
3
Chapter 4 Autonomic Pharmacology
1 cholinergic fibers include :
(1) all (parasympathetic and sympathetic) preganglionic efferent autonomic fibers and
somatic motor fibers to skeletal muscle.
(2) all parasympathetic postganglionic fibers
(3) a few sympathetic postganglionic fibers, the fibers innervate to sweat gland and
skeletal muscle vascular dilating nerves
(4) the nerve innervate to adrenal medulla
2 adrenergic fibers: most of the sympathetic postganglionic fibers
3 coupling mechanism of receptor-effect
β receptor combines with Gs, Gs, activates AC, cAMP activates protein kinase which
activates phosphoslation.
α2 receptor combines with Gi and inhibits AC activity , decreases cAMP.
α1 receptor couples with GP, activates PLC.
4 M effect
Heart: rate↓ cardiac contractility↓ conduction↓
Blood vessel: dilation, blood pressure↓
Eye: pupil constriction, intraocular pressure↓ ciliary muscle constriction
Salivary gland: secretion
Viscera: bronchi constriction, gastrointestinal movement ↑
5 adrenergic effect
Heart:β1 rate↑ contractility↑ conduction↑Bp↑
Blood vessel:
Coronary: α1, α2 constriction, β2 dilation
Muscle
β2 dilation
Veins:
α1, α2 constriction, β2 dilation
Viscera: bronchi β2 dilation
Eye: α1 pupil dilatation ,
autonomic[]自主的
Cholinergic[]
skeletal
[] 骨骼的
Preganglionic [] 节 前 的
efferent
[] 传出的
parasympathetic[] 副 交 感 的
innervate
[] 神经支配
intraocular[] 眼 内 的
ciliary
[] 睫状的
salivary[i] 唾液
viscera [] 内
脏
gastrointestinal [] 胃肠的
4
Chapter 5 Cholinoceptor-activating and
Cholinesterase -Inhibiting Drugs
1 M-cholinoceptor agonists
pilocarpine
pharmacological effects:
Eye: miosis, papillary constrictor muscle
decrease intraocular pressure
cyclospasm(spasm of accommodation), contraction of ciliary muscle
Glands：increase secretion of sweat gland and salivary gland
Uses: glaucoma, iritis(prevent iris to lens)
2 cholinesterase inhibitors
cholinesterases divides into acetylcholinesterase(AchE) and pseudocholinesterose.
The former is highly concentrated at neuromuscular junction, the later is present
primarily in plasma and liver. Cholinesterase inhibitor will express M and
N-cholinergic effects.
3 Neostigmine(reversible)
pharmacologic effects: cholinesterase inhibitor effect and direct activating N2 receptor
clinical use: myasthenia gravis
postoperative ileus and urinary retention: neostigmine excites GI tract
smooth muscle and bladder detrusor
paroxysmal supraventricular tachycardia: decrease heart rate.
Overdosage of muscle relaxants: tubocurarine, but prohibit to use for
succinylcholine intoxication.
Side effects: nausea, vomiting, abdominal pain, tachycardia, fibrillation of muscle
fibers, cholinergic crisis.
Contraindications: mechanical intestinal obstruction, urinary obstruction, bronchial
asthma
miosis [] 瞳 孔 缩 小
cyclospasm 调 节 痉 挛
papillary[]乳突的
glaucoma [] 青 光 眼 iritis [] 虹 膜 炎
ciliary[]睫状的
myasthenia gravis [] [] 重症肌无力
ileus [] 肠梗阻
urinary [] 尿液的 asthma
[] 哮喘
retention []渚留
detrusor[] 逼尿肌
supraventricular 室上性
tachycardia[] 心动过速
tubocurarine [] 筒 箭 毒 碱
Contraindications 禁忌症
succinylcholine[] 琥 珀 酰 胆 碱
obstruction[]梗阻
paroxysmal[] 阵 发 性 的
pilocarpine
[




] ]毛
果 芸
香 碱
5
Chapter 6 Organophosphates Anticholinesterase Intoxication and
Cholinesterase Reactivators
1 mechanism of intoxication: organophosphates combine with cholinesterase to form
complex, then “aged” phosphorylated cholinesterase.
2 acute intoxication
M signs and symptoms: miosis, salivation, increase bronchial secretion, sweating,
bronchoconstriction, vomiting, diarrhea, bradycardia, hypotention.
N actions: involuntary twitchings
3 treatment of acute intoxication: atropine antagonize M symptoms. Cholinesterase
re-activator(pyraloxime methoiodide, PAM; prelidoxime chloride, PAM-CL) is
capable of regenerate active enzyme from the organophosphorus-cholinesterase
complex and also antagonize the twitching.
diarrhea [] 腹泻
twitchings [] 颤搐
6
Chapter 7 Anticholinergic Drugs (M antagonist)
Anticholinergic drugs can combine with cholinergic receptors and inhibit Ach or
cholinergic drugs to combine with the receptors. They are divided into
M-cholinoceptor blocking drugs and N-cholinoceptor blocking drugs.
M –receptor antagonist:atropine—non selectively M receptor antagonist
1 pharmacological effects:
Glands: inhibit the secretion of salivary gland, sweat gland and bronchial secretory.
Eye: pupil dilation, increase intraocular pressure, cycloplegia
Smooth muscle: relaxation of viseral smooth muscle, stomach and intestine , bladder
detrusor and urinary tract smooth muscle and weak effect on biliary tract and uterus.
Cardiaovascular system : increase HR, dilate blood vessel , Bp decrease and
improve microcirculation.
CNS: stimulating effect.
2 clinical uses:
visceral colic: gastric and intestinal colic pain and bladder irritating symptoms.
Combined with pethidine for treatment of gallbladder colic and renal colic pain
preanaesthetic medication ， ophthalmologic disorders , bradycardia
anti-shock especially for infectious shock. Organophosphate intoxication.
salivary[] 唾液的
intestine[] 肠
cycloplegia
[]
调
节
麻
痹
detrusor[] 逼尿肌
colic
[]
绞 痛
urinary[]
尿 的
biliary[]胆汁的
gallbladder [] 胆 囊
ophthalmologic
[] 眼科的
preanaesthetic medication 麻醉前给药
pethidine 度冷丁
uterus[]子宫
bradycardia [] 心动过缓
visceral[]
内脏的
7
Chapter 8 Adrenergic Drugs
Adrenergic drugs are a group of drugs, which have similar chemical structures and
pharmacological actions. They may combine with and activate adrenoceptors and
produce adrenomimetic effects, they are called adrenomimetic drugs. These drugs are
amines, their effects are similar to that of exciting sympathetic nerves, thus they are
also called sympathomimetic drugs.
1 mixed α and β agonists: adrenaline(epinephrine)
1.1Pharmacological effects:
(1) Cardiovascular system:
blood vessel: α constrict mucous membranes and skin vessels.
Constrict renal and mesenteric blood vessel
β2 dilate vessel of skeletal muscle, coronary
heart: a powerful stimulant effect on heart
β1 HR↑（positive chronotropic effect）
contraction↑(positive inotropic effect)
conduction↑ increase the secretion of renin
Bp: small dose or therapeutic dose increases systolic and diastolic，.
(2)Smooth muscle: relaxation of most kinds of bronchial smooth muscle
(3)Metabolic effects: hyperglycemia
1.2 Clinical uses
Cardiac arrest:
Anaphylaxis: anaphylactic shock
Bronchial asthma:
Local application: use with local anesthetics to constrict the regional blood
vessels
1.3 Side effects: restlessness, anxiety, insomnia, palpitation, sweating, very high
dose :severe headache, elevation of BP, the danger of cerebral
hemorrhage, arrhythmia and ventricular fibrillation
1.4 Contraindications: hypertension, sclerosis of cerebral artery, ischemic heart
disease, congestive heart failure, hyperthyroidism. and diabetes.
2 α receptor agonist: norepinephrine, NA
It has very strong α receptor activating effect,
2.1 pharmacological effects:
(1) very strong blood constriction α1 receptor. NA has relatively little effect on
β2, dilation of coronary blood vessels, increase coronary blood flow.
(2) heart: mild activation on heart(β1), increases cardiac contractility, cardiac
8
output, heart rate, conduction
(3) Blood pressure: increase systolic and diastolic pressure.
2.2 clinical uses
(1) hypotension induced by drug intoxication( chlorpromazine, A is
contraindicated))
(2) early phase of neurogenic shock
(3) upper gastrointestinal tract bleeding
3 β receptor : isoprenaline(isoproterenol)
3.1 pharmacological effects: β1, β2 receptor agonist
(1) cardiovascular system :positive inotropic and chronotropic effects, conduction
increase, diastolic pressure falls, systolic blood pressure may remain
unchanged or rise, mean arterial pressure falls.
(2) bronchial smooth muscle: relaxation
3.2 clinical uses
(1) cardiac arrest and heart block (2) asthma
(3) shock: now seldom used
4 DA activates DA receptor, β1 and α receptor. DA causes an increase of cardiac
contractility. It also causes the release of NA from nerve endings, in induces
vasoconstriction(α1).it elevates BP and has weakβ2 effects. The effect on D1
receptor of kidney, and mesentery induces dilation of renal and mesenteric blood
vessels.
Adrenomimetic 拟肾上腺素
cutaneous []
皮肤的
mesenteric[]
肠
系
膜
的
metabolic[] 代谢
systolic[] 收缩的
sclerosis [] 硬
化
diastolic 心脏舒张的
ischemic 缺血
hemorrhage
[]
出 血
hyperglycemia
[] 高血糖症 arrhythmia [] 心
律失常
ventricular [] 心室的
fibrillation
[]
心 室 纤 维 颤 动
diabetes[]糖尿病
hyperthyroidism [] 甲亢
hypotension [] 低血压
9
Chapter 9 Adrenoceptor Blocking Drugs
1 α－adrenoceptor blocking drugs
Non selective α－receptor blocking drugs: phentolamine
Pharmacological effects: decrease peripheral resistance, dilate blood vessel, decrease
BP, weak cardiac stimulation effect. After pretreatment with α-antagonist, Adr(E)
shows its decrease of BP, which is called “epinephrine reversal”.
Clinical uses: peripheral vascular diseases such as Raynaud’s Syndrome,
thromboangitis) , excess local vasoconstrictor, anti-shock,
pheochromocytoma, myocardiac infarction and stubborn congestive
heart failure.
Side effect: hypotension
Phentolamine should be used with particular caution in patients with coronary artery
(because of its reflex cardiac stimulation) or a history of peptic ulcer( agonist at
M and H2 receptor which increase the gastric acid release)..
α1 receptor blocker: prazosin, it is effective in the management of hypertension with
less tachycardia than occurs in phentolamine.
2 βreceptor blocking drugs
Non selective : propranolol, pindolol, sotalol, timolol
Pharmacological effects:
(1)β blocking effects: heart: decrease HR, cardiac contractility and cardiac output,
slowed AV conduction.(negative chronotropic and inotropic), hypoglycemia
blood vessel: weakly increase peripheral resistance. Inhibit release of renin
Decrease BP,
lead to bronchoconstriction
(2) endogenous sympathomimetic effect: (pindolol)
(3) membrane stabilizing action:
(4) other effects: anti-platelet aggregation
Clinical uses: angina pectoris(in stable and unstable not in variant because of
coronary constriction ) , cardiac arrhythmias, hypertension, glaucoma(timolol
reduces the production of aqueous humor)
Selective β1 antagonist: atenolol, metoprolol
3 αand β antagonist: labetalol
pheochromocytoma [] 嗜 铬 细 胞 瘤
renin [] 肾素 endogenous [] 内源性的 platelet
[]血小板
aggregation [] 聚集 angina pectoris [] 心
绞痛
arrhythmia [] 心律失常
10
Chapter 10 Sedative-Hypnotics
Hypnotics are drugs used to produce drowsiness and sleep, while sedatives are used to
calm anxious and restless patients.
1 Benzodiazepine: diazepam
Pharmacological effects:
(1) Anti-anxiety, (2) sedation hypnosis(prolong stage 2 NREM sleep. Shorten3,4
NREM, weakly shorten REM), (3) anti-convulsant effect and anti-epileptic effects.(Bz
combines with Bz receptor, strengthen the function of GABA. (4) central muscle
relaxation
Clinical uses: sedative and anti-anxiety, insomnia, tetanus, convulsion induced by fever
and drug intoxication, relieve muscle spasm. Antagonist of Diazepam is flumazenil.
Bz has no anesthetic effect.
Mechanism: Benzodiazepine(BDZ) receptors appear to be located in GANA A receptor
sites. BDZ combine with GABA-BDA receptor –chloride ion channel complex and
potentiate the effect of GABA.
Adverse effects: drowsiness, fatigue, dizziness, tolerance, dependence, addiction
2 barbitutates:
Pharmacological effects: sedation, hypnotics(prolong stage Ⅱ NREM sleep, shorten
REM), anti-convulsant effect and anti-epileptic effects, anesthesia, used for anxiety,
epilepsy, anesthesia , pre-anesthetic medication.
Mechanism: barbiturates have combining point on GABAA receptor-Cl- complex. After
combing with the complex, they enhance the binding of GABA to GABA A receptors.
Increase the duration of Cl- channel openings. Then increase Cl- influx, induce
hyperpolarization.
More and strong side effect: hangover, rebound, tolerance, dependence, addiction
insomnia [] 失 眠 tetanus [] 破 伤 风 convulsion
[]
惊厥 anaesthetic [] 麻醉的 dizziness [`] 头昏
眼花
influx [] 流 入
hyperpolarize[]
( 使) 超极化
11
Chapter 11 Antiepileptic Drugs
1 classification of seizure type：
Partial seizures: simple; complex; psychomotor.
Generalized seizures: grand mal; absence(petit mal)
Status epilepticus
2 antiepileptic drugs
2.1 phenytoin: is a weak acid, an enzyme inducer. At low dose, the elimination is
according to first order kinetics. At high dose, it is according to zero order kinetics.
Pharmacological effect and mechanism: it has a broad range of action against most
types of seizures(grand mal and psychomotor epilepsy) except absence seizures. The
major action of phenytoin is to block sodium channels.
Clinical uses: antiepilepltic; trigeminal neuralgia,;antiarrhythmia
Side effects: dose-related adverse effect such as nystagmus, diplopia, ataxia
Chronic toxicity: gingival hyperplasia, hypocalcium , folate efficiency,
Allergic reaction: AA, platelet decrease,
Teratogenicity: fetal hydantoin syndrome
2.2 phennobarbital: it is used to prevent and treat grand mal, psychomotor epilepsy,
simple partial seizure and status epilepticus, but is not indicated in the treatment of
absence seizures. Mechanism: block calcium channel, enhance GABA-mediated
inhibition, inhibit excitatory of glutamate.
3 selectivity of antiepileptic drugs
Grand mal: carbamazepine, Phenobarbital, phenytoin, sodium valproate
Petit mal: clonazepam, ethosuximide, sodium valproate
Psychomotor:carbamazepine, phenytoin, Phenobarbital, sodium valproate
Status epilepticus: diazepam IV, lorazepam IV, phenytoin IV, Phenobarbital IV.
4 anticonvulsant drugs: barbiturates, chloral hydrate, diazepam and magnesium sulfate.
Mg2+ has direct depressant effect on skeletal muscle. Decrease BP, the action of Mg2+
on neuromuscular function are antagonized by Ca2+
seizure[] 发作
grand mal 大发作 petit mal 小发作 fetal[]
胎儿的
status epilepticus [] 癫痫持续状态 phenytoin[]苯妥
英
trigeminal[]
三
叉
神
经
的
nystagmus[]眼球震颤
diplopia[]复视
失调
gingival[]齿龈的
teratogenicity[]
eclampsia[]惊厥
glutamate[] 谷氨酸盐
酸盐
anticonvulsant[].
magnesium[]镁
ataxia[]共济
folate[]叶酸
致
畸
性
sulfate[] 硫
抗
惊
厥
药
12
Chapter 12 Antipsychotic Drugs
General introduction: The term psychosis denotes a varity of mental disorders.
Schizophrenia is a particular kind of psychosis characterized by a clear sensorium but
a marked thinking disturbances. Antipsychotic drugs are also called neuroleptics,
which have been used mainly for treating schizophrenia but are also effective in some
other psychosis and agitated states.
The dopamine theory for schizophrenia: excessive dopaminergic activity underlies the
disorder.
Four important dopaminergic system and pathways:
Meso-limbic, meso-cortical pathway which has connection with emotions.
Nigrostriatal pathway is involved in the coordination of voluntary movement.
Tuberoinfundibular system is involved in the secretion of hormone.
1 chlorpromazine, wintermine: a potent dopamine receptor antagonist.
1.1 Pharmacological effects:
Antipsychotic effect:
Anticholinergic and antiadrenergic effects
Temperature regulation
Antiemetic effects
Endocrine effects
1.2 Clinical uses: psychotic disorder; nausea and vomiting; hypothermic anesthesia;
artificial hibernation
1.3 Side effects:
Extra-pyramidal system reactions: parkinson’ syndrome, akathisia, acute dystonia
reactions, tardive dyskinesia
Cardiovascular effects: orthostatic hypotension
Autonomic side effects: atropine-like effects
Metabolic and endocrine side effects
Allergic reactions
Ocular side effects
2 anti-manic drugs
Etiology of mania and depression is supposed by “amino theory”, “amino theory”
supposed that symptoms of manic are induced by large amount of catecholamines in
CNS and that depression is induced by lack of catecholamines in CNS. Lithium
carbonate is effective in mania. It may control the symptoms of insomnia, excitement,
improve the emotional disorders.
13
Clinical uses: the prevention of bipolar manic-depressive and the treatment of acute
mania.
3 antidepressants: tricyclic , tetracyclic, selective 5-HT reuptake inhibitors
pyramidal []锥体的
akathisia[] 静坐
不能
dystonia[] 肌张力障碍 tardive[] 迟缓的
dyskinesia[]
运
动
障
碍
orthostatic[] 直立的
mania[] 狂躁
tricyclic[]三环
的
tetracyclic[]四环的
14
Chapter 13 Analgesics
Narcotic analgesics are also called opioid analgesics, analgesia is the relief of pain
without the loss of consciousness. Opioid is the generic term for the morphine-like
activity that reduces pain and induces tolerance and physical dependence. Opioids
interact with opioid receptors, mimic the effects of endogenous opiopeptins.
1 morphine
1.1 pharmacological effects
CNS: analgesia and sedation; respiratory depression; nausea and vomit; inhibition of
cough refax; miosis.
Cardiovascular system: inhibit the vasomotor center causing peripheral vasodilation,
inducing hypotension. Increase histamine release, Pco2 causes cerevral vasodilation,
increased intracranial pressure.
Smooth muscle: constipation, urinary retention, increased biliary pressure
Clinical uses: (1) analgesia, for severe pain and pain of terminal illness, such as trauma,
burn, cancer, acute myocardial infarction. For renal or biliary colic, use morphine with
atropine. (2) cardio-genic asthma, acute pulmonary edema with left ventricular failure
(3) diarrhea
Tolerance , physics dependence
Morphine poisoning: coma, slow respiration and pinpoint pupil
2 codeine: is an analgesic, used for antitussive
3 fentanyl: it has 80 times the analgesic potency and respiratory depressant properties
of morphine. Shorter duration of action , weak addiction. Used for acute pain,
combined use with anaesthetics to decrease the dosage of anaesthetics.
4 methadone: less severe withdrawal syndrome than morphine and often substituted
for other opioids for treatment of physical dependence. It is a useful drug for
detoxification and for maintenance of the chronic replacing heroin addict.
5 opioid antagonists: naloxone, block the action of endogenous opioid peptides as
well as morphine-like drugs, relief the respiratory depress, alcohol toxic, infectious
shock , induce abstinence syndrome.
analgesic[] 止痛剂
opioid 鸦片
endogenous[] 内 生 的
intracranial
[] 颅内的
constipation [] 便 秘
retention
[] 渚留
biliary [] 胆囊的
colic [] 绞痛
pulmonary [] 肺部的
edema []水肿
肺水肿
diarrhea [] 痢 疾 , 腹 泻
antitussive
[] 镇咳药
anaesthetic [] 麻醉药
abstinence[]
戒断
15
Chapter 14 Antipyretic-Analgesia and Anti-inflammatory
Introduction:
The effectiveness of NSAID is due to their ability to inhibit cyclo-oxygenase
(prostaglandin synthase), which catalyzes the conversion of arachidonic acid to
endoperoxide compounds. At appropriate doses, the drugs decrease the formation of
both the prostaglandins and thromboxane A2 but not the leukotrienes.
Aspirin and other drugs are referred to as non-steroidal anti-inflammatory drugs. The
mechanism is that they inhibit cox, inhibit the synthesis of prostaglandins.
1 aspirin: antipyretics effect; analgesic effect; anti-inflammatory, antirheumatic，
inhibition of platelet aggregation.
Clinical uses: fever ; headache, toothache; rheumatic fever; small daily dose of aspirin
for prophylaxis of thrombus, embolism, stroke and cardiac infarction.
Side effects: gastrointestinal tract; coagulation disorders; hypersensitivity; salicylism;
reye’s syndrome .
2 Acetaminophen: is the active metabolite of phenacetin responsible for its analgesic
effect. It has antipyretic, analgesic effects, weak antiinflammatory and antirheumatic
effect. Phenacetin can no longer be prescribed in China, but is still used in some
analgesic combinations.
Prostaglandin [] 前列腺素 catalyze[]
催化
antipyretic []
退 热 的
analgesia
[] 镇痛药
thrombus[]血栓
embolism[] 栓塞
coagulation[] 凝结
arachidonic acid 花生四
烯酸
leukotrienes 白三烯
acetaminophen []醋氨酚,对乙酰
氨基酚
phenacetin [] 非那西汀(解热镇痛剂的一种)
antirheumatic [] 治疗风湿药剂
prophylaxis [] 预防
16
Chapter 15 Renin- Angiotensin System
Angiotensin Ⅱ is a potent direct vasoconstrictor. It stimulates the secretion of
aldosterone, which promotes sodium and water retention. Captopril is a specific
competitive inhibitor of ANG Ⅰ converting enzyme, thus captopril inhibits
vasoconstriction and inhibits sodium and water retention and slightly increases serum
potassium levels. Because ACE is necessary to catalyze the degradation of
bradykinin, captopril may increase the concentration of bradykinin, which is a potent
vasodilator.
Captopril lowers blood pressure principally by decreasing peripheral vascular
resistance. Cardiac output and heart rate are not significantly changed. Unlike direct
vasodilators, captopril does not result in reflex sympathetic activation and can be used
safely in persons with ischemic heart disease. The absence of reflex tachycardia may
be due to downward resetting of the baroreceptor or to enhanced parasympathetic
activity.
Clinical uses: hypertension, severe heart failure.
ARB:
Losartan, a kind of non-peptide angiotensin Ⅱ receptor antagonist. It is a selective
and competitive AT1 antagonist.
Baroreceptor [] 压力感受器
parasympathetic [].副交感神经
17
Chapter 16 Anti- Arrhythmia Agents
The cardiac arrhythmias are abnormalities in the rate, rhythm, or site of origin of
cardiac impulse , or disturbance in the conduction of cardiac impulse ,or both of them.
1 calssification of antiarrhythmic drugs:
Ⅰ a: moderate Na+ channel blocking drugs, K+,Ca2+also blocked, quinidine,
procainamide.
Ⅰb: mild Na+ channel blocking drugs, K+ efflux facilitating drugs, lidocaine,
phenytoin.
Ⅰc: severe Na+ channel blocking drugs, propafenone
Ⅱ: β－adrenergic blocking drugs: propranolol.
Ⅲ: prolongation of APD and Na+, Ca2+ channels blocking drugs, amiodarone
Ⅳ: Ca2+ antagonists, verapamil,
2 clinical uses:
Quinidine is a broad-spectrum anti-arrhythmia drugs, used in the supra-ventricular
arrhythmias, tachycardia, atrial flutter, atrial fibrillation. In these cases digitalis may
be added together with quinidine. Used in ventricular arrhythmias, such as ventricular
premature depolarization, tachycardia.
Lidocaine: is a local anesthetic agent and also an anti-arrhythmic drug.
Lidocaine is very effective against the ventricular arrhythmias caused by acute
myocardial infarction, digitalis toxicity. This drug is first used to prevent and treat the
acute myocardial ischemia. It is rarely used in supra-ventricular arrhythmias.
Phenytoin: is an antiepileptic drug and also an anti-arrhythmic drug. It is superior
against digitalis-induced arrhythmias to lidocaine.
Propranolol: is mainly used in supra-ventricular arrhythmias and ventricular
arrhythmias induced by enhanced catecholamines.
Amiodarone is a broad spectrum anti-arrhythmic drug.
Verapamil: is first used in converting reentrant paroxysmal supra-ventricular
tachycardia to normal sinus rhythm. It is rarely used for ventricular arrhythmias.
tachycardia[] 心动过速
atrial flutter 心房扑动，
atrial fibrillation 心房颤动
premature depolarization 早搏
catecholamines 儿茶酚胺类
reentrant 折返
paroxysmal []发作性的,
18
Chapter 17 Diuretics and Osmotic Diuretics
Diuretics drugs acting on renal tubules increase urine flow and NaCl excretion, which
are useful in clinical conditions to remove edema, and also used to treat some
unedema diseases.
High efficacy diuretics(loop diuretics): furosemide, ethacrynic acid.
Acting on thick ascending limb of loop, inhibit Na+-K+-2Cl- cotransport system, its
diuretic activity is rapid, strong and short. Large amounts of Na+,K+,2Cl-, and Ca2+,
Mg2+ are excreted. Increase renal blood flow , increase rennin release, relieve
pulmonary congestion and reduce left ventricular filling pressures. Induce ototoxity.
Uses: acute pulmonary edema and brain edema; acute and chronic renal failure;
hypertension crisis; de-toxication
Side effects:
electrolyte disturbance: hypokalemia, hypomagnesemia, hypochloremic, hypocalcium.
Ototoxity; hyperuricemia;
Moderate efficacy diuretics(thiazides ): hydrochlorothiazide
The site of action of thiazide diuretics is at the distal convolute tubule, they inhibit the
Na+--2Cl- cotransport,.
Uses: edema, hypertension, anti-diuretic
Side effects:
electrolyte disturbances: hypokalemia, magnesium deficiency.
Hyperuricemia; hyperglycemia and hyperlipidemia.
Low efficacy diuretics(potassium –sparing diuretics):
These drugs reduce Na+-K+ exchange,
Spironolactone
is a competitive antagonist to aldosterone, used for
edema,hypertension, congestive heart failure. triameterene, amiloride
Osmotic diuretics: mannitol
These agents are small molecular weight substances,
Pharmacological effects: dehydration, increase urine volume, dilate renal vascular.
Uses: brain edema, glaucoma, prevent acute renal failure,.
Oto-toxity. oto-[] 耳的
de-toxication 毒物排泄
edema[]水肿
Cotransport 共转运子
electrolyte
[]
电
解
aldosterone[] 醛固酮
质
19
Chapter 18 Anti-hypertensive Drugs
According to the WHO standard on 1997, normal blood pressure should not exceed
140/90 mmHg. Hypertension can be classified into primary and secondary according
to etiology. Long term hypertension can damage the blood vessel, induce hypertrophy
of left ventricle, arterial sclerosis, myocardial infarction, cardiac failure; cerebral
bleeding, thrombus, embolism; renal failure.
1 classification of antihypertensive drugs:
Affecting blood volume: diuretics, thiazides
ACEI and ARB: captopril, losartan.
β－antagonist: propranolol
CCB: amlodipine.
Anti-sympathetic drugs:
Centrally acting agents: clonidine.
ganglionic blocking drugs : mecamylamine
adrenergic neuron blocking agents :reserpine
adrenergic receptor antagonist: α1- receptor antagonist
prazosin
α, β - receptor
antagonist labetalol.
Vasodilators:
directly vasodilators: hydralazine, nitropruside
indirectly: potassium channel openers : minoxidil, diazoxide
2 mechanism of antihypertensive drugs
Diuretics: the early hypotensive effect is related to a reduction in blood volume and
cardiac output; the long-term effect os related to a reduction in peripheral vasculature
resistance.
ACEI: decrease the formation of ANGⅡ, decrease the effect of ANGⅡ; increase the
concentration of bradykinin, increase the effect of bradykinin. ARB blocks the
AT1 receptor.
β－antagonist: blockβ1, inhibit myocardial contractility, decrease output; decrease
the secretion of renin.
CCB: negative inotropic effect, decrease output. inhibit the calcium influx into arterial
smooth muscle cells, dilate artery.
Clonidine: acting on central α and imdiazoline receptor.
ganglionic[]
神
bradykinin[]缓激肽
inotropic[]肌力的
经
节
的
Imdiazoline 咪唑啉，
20
Chapter 19 Drugs for Congestive Heart Failure
Congestive heart failure occurs when the cardiac output is inadequate to provide the
oxygen needed by the body. It is a highly lethal condition. Clinical research has
shown that therapy directed at non-cardiac targets may be more valuable in the
long-term treatment of congestive failure than traditional positive inotropic agents.
Thus, drugs acting on the kidneys have been considered at least as valuable as
digitalis for this condition. ACEI and vasodilators have come into common use.
Cardiac glycosides:
Pharmacological effects:
Positive inotropic effect: increase the contractility of myocardium, increase the
cardiac output in patient with CHF, decrease the myocardial oxygen consumption.
Negative chronotropic effect: slow the heart rate in the patients with CHF. Increase
the vagal tone of the heart, prolong the refractory period of the A-V node and decrease
conduction velocity through the A-V node.
Diuretics.
Mechanism: inhibit the Na+-K+-ATPase,
Clinical uses: congestive heart failure, atrial fibrillation, atrial flutter, paroxysmal
supraventricular tachycardia.
Adverse reaction:
cardiac side effect: Premature ventricular beats, ventricular tachycardia and fibrillation,
atrioventricular block, sinus arrhythmia and S-A block, bradycardia.
Extra-cardiac effect: GI tract; CNS; visual changes;
Treatment of toxic effect: potassium chloride; phenytoin and lidocaine can be treat
ventricular tachycardiac.
vagal[] 迷走神经的
atrial 心房的
paroxysmal []发作性的, 突发性的
21
Chapter 20
Anti-Angina Pectoris Drugs
Angina pectoris is a common symptom of coronary artery disease caused by transient
episodes of myocardial ischemia and anoxia, but some time also by “silent”
myocardial ischemia in the absence of symptoms. Angina pectoris results from an
imbalance between oxygen supply-demand relationship in ischemic regions of the
myocardium.
1 nitrates and nitrites：nitroglycerin, isosorbide dinitrate
Pharmacological effects:
Relaxation of vascular smooth muscle, decrease oxygen demand; redistribution of
myocardial blood;
Uses: acute angina pectoris attack, prophylaxis of angina pectoris ; treatment of acute
myocardial infarcion; congestive heart failure
2 β-adrenergic receptor blockers
Pharmacological effects:
The effect of β-adrenergic receptor blockade; improvement of blood supply in
ischemic areas
Clinical uses: stable angina, not in variant
3 calcium channel blockers
Pharmacological effects
Reduction of myocardial oxygen demand; dilation of coronary vessels; protection to
ischemic myocardial cell
Clinical uses: varient angina with AMI
Episode [] 事件
myocardial [] 心
肌 的 ischemia 缺 血 anoxia [] 缺 氧 症
nitrates 硝 酸 盐
nitrites 亚 硝 酸 盐 nitroglycerin [] 硝 化 甘 油
prophylaxis [] 预防
Variant [] 变异性
22
Chapter 21 Drugs Acting on the Blood and Blood Forming Organ
Introduction: The physiological system that control blood fluidity are both complex
and elegant. Blood must remain fluid within the vasculature and clot quickly when
exposed to nonendothelial surfaces at sites of vascular injury. When intravascular
thrombi do occur, a system of fibrinolysis is activated to restore fluidity. In normal
situation, a delicate balance prevents both thrombosis and hemorrhage and allows
physiological fibrinolysis without excess pathological fibrinolysis. The drugs
described in this chapter achieve the aim: to alter the balance between procoagulant
and anticoagulant reactions.
1 anti-coagulant drugs
Heparin: is discovered by a medical student, J Mclean, working at John Hopkins
Medical School in 1916. Seeking to devoted one year to physiological research he
was set to study the thromboplastic substance in the body. He found that extracts of
brain, heart and liver accelerated clotting, but that activity deteriorated during storage.
To his surprise, the extract of liver which he had kept longest not only failed to
accelerate but actually inhibit clotting.
Heparin is rapidly effective, acts for only a few hours and must be given parenterally.
Heprin is active in both extracorporeal and intracorporeal.
Mechanism:Heparin depends for its actions on the presence on plasma of a protein,
anti-thrombinⅢ， which is a naturally inhibitor of thrombin and of active factors Ⅸ，
Ⅹ，Ⅺ，Ⅻ with serine residue. In the presence of heparin anti-thrombin becomes
vastly more active.
Pharmacological effects:Heparin is effective in low dose to prevent thrombin formation,
in high dose to stop extension of a thrombin; inhibit the proliferation of vascular
smooth muscle cells and involve in angiogenesis;inhibit certain aspects of the
inflammatory response.
Clinical practice: treatment of established thrombosis such as pulmonary embolism ,
deep venous embolism, cerebral embolism.; prevention of thrombosis such as
postoperatively, after myocardial infarction.
Fluidity [] 流动性 elegant [] 精确的 clot
[] 凝块 intravascular [] 血管内的 thrombi
[] 血栓症 fibrinolysis
[] 纤维蛋白溶解 delicate[] 精致的
hemorrhage
[]
出
血
procoagulant
[] 促凝血的
parenteral
[]
肠
胃
外
的
extracorporeal
[] 体外的
intracorporeal 体 内 的
thrombin [] 凝 血 酶
serine
[]丝氨酸
pulmonary [] 肺部的 embolism [] 栓塞
23
Chapter 22 Histamine-Receptor Antagonist
Introduction: Histamine is an autacoid from mast cell and basophile, it involves in
hypersensitive reaction. Histamine receptor has three subtypes. They are found in
peripheral tissues and the central nervous system. Skin , the mucosa of the bronchial
tree, and the intestinal mucosa contain large numbers of mast cell.
1 H1-receptor antagonist
Physiological effects: antagonize the peripheral effects induced by H1 including
contraction of bronchi, gastrointestinal, uterus, blood vessel dilation, high
permeability, blood pressure decrease; some drugs have sedation, hypnotic and
anti-vomit effects, some can stimulates CNS. Some have anti-cholivergic effects.
Clinical practice: hypersensitive disease, motion sickness and vomit.
2 H2-receptor antagonist: includes cimetidine, ranitidine, Cimetidine is a cytochrome
P-450 enzyme inhibitor. It inhibits the secretion of gastric acid induced by H2, used for
peptic ulcer.
autacoid [] 自体活性物质 mast [] 肥大
basophilic
[]
嗜 碱 的
hypersensitive
[] 敏感的
peripheral [] 外周的
mucosa []黏膜
bronchial []支气管的
intestinal [] 肠内的
gastrointestinal
[]
胃 与 肠 的
uterus
[] 子宫
motion sickness 晕动病 peptic [] ulcer [] 胃溃疡
24
Chapter 23 Drugs Acting on Respiratory System
Introduction: Asthma is an inflammatory illness with bronchial hyperreactivity and
bronchospasm . pathological reaction: inflammatory cells such as eosiniphil,basophil,
T lymphocyte, macrophage, mast cell; mediators such as LT, cytokines, histamine,
involve in the inflammtory, induce epithelial shedding, bronchoconstriction, tissue
damage, mucous secretion. Treatment : inhibit the infalmmatory; bronchidilation.
1 glucocorticoids
Pharmacological effects:
anti-inflammatory : inhibit the production of cytokines such as IL, TNF and mediators
such as LT, PG. . Some cytokines and mediators can activate inflammatory cells.
Clinical practice: systemic glucocorticoids are used for acute asthma exacerbations and
chronic, severe asthma, but bring many side reactions, inhaled glucocorticoids has
little side reaction. Drug: beclomethasone
2 bronchial dilation
β-adrenergic receptor agonists:
adrenaline: agonize α-receptor, induce mucosa vascontriction, decrease edema, β
2-receptor induce bronchodilation, adrenaline is given subcutaneous injection.
asthma [] 哮喘
inflammatory [i] 炎症的
Eosinocyte [] 嗜酸性粒细胞 basophil []
嗜碱细胞
macrophage [] 巨噬细胞 cytokines 细胞因子
epithelial [] 上皮的 shedding [] 脱落 IL 白介
素，
TNF 肿瘤坏死因子 systemic [] 全身的 glucocorticoids 糖皮质激
素
exacerbation [] 恶化 inhale [] 吸入
beclomethasone [] 氯 地米 松 , 倍氯 米 松 edema
[] 水肿
25
Chapter 24
Drugs Acting on Digestive System
Introduction:
Attack factors to gastric mucosa: gastric acid; proteinase; H.Pylori
Defensive factors: mucus; bicarbonatic ion, PG.
Aim : keep the balance between attack factors and defensive factors, promote healting,
prevent recurrence.
1 antacids: increase the pH of gastric, decrease the activity of proteinase.
Magnesium hydroxide Mg(OH)2
side effect: diarrhea
Aluminum hydroxide Al(OH)3
constipation
Calcium carbonate
CaCO3
abdominal distension
Sodium bicarbonate
NaHCO3
2 inhibit the secretion of acid
R
Agonist
Antagonist
M1
Ach
Pirenzepine
H+-K+-ATP Omerprazole
H2
Histamine
Cimetidine
G
Gastrin
Proglumide
3 mucosa protecting agents
Prostaglandin analogues: misoprostol
Sucralfate
Bismuth potassium citrate
4 anti-HP drugs
Amoxycilin, tetracycline, clarithromycin, metronidazole
Mucosa [] 黏膜 proteinase [] 蛋白酶
mucus [] 粘液 bicarbonate [] 重碳酸
盐
recurrence [] 复发 diarrhea [] 腹泻
constipation
[]
便
秘
prostaglandin
[] 前列腺素
abdominal distension [][] 腹气胀
analogues [] 相似物 misoprostol 米索前列醇 Sucralfate 硫糖铝
Bismuth potassium citrate 枸橼酸铋钾
26
Chapter 25
Adrenocortical Hormones
Adrenal cortex release a large number of steroids into the circulation, including
glucocorticoid(GCS), and gonadal hormones.
1 physiological roles if GCS
Hyperglycemia: increase glycogen synthesis and gluconeogenesis, inhibit uptalk of
glucose from muscle cells.
Decrease protein synthesis
Accelerate lipolysis and inhibit lipogenesis
Increase sodium reabsorption and potassium loss
2 pharmacological effects
Anti-inflammatory; immunosuppression; anti-toxicity ; anti-shock; effect on CNS
3 clinical use
Substitution therapy; severe infections or inflammation; autoimmune disorders and
allergic disorders; shock; hematologic disease; local applications
4 toxicity / side effects and contraindication
(1)Induced by using GCS with large doses for long time : Cushing’s syndrome; induce
hidden infections or exacerbate infection; psychosis; glaucoma; growth retardation in
children; electrolytic disorder such as hypokalemic; osteoporosis
（2）withdrawal of steroid therapy rapidly or stop abruptly
Adrenal [] 肾 上 腺 的
cortex [] 皮 层 steroid
[] 类固醇
glucocorticoid []糖皮质激素
mineralocorticoids [] 盐 皮 质 激 素 gonadal
[] 性腺
glycogen
[]
糖
原
gluconeogenesis
[] 糖异生
lipolysis [] 脂解 lipogenesis [] 脂
肪生成
sodium [] 钠 potassium [] 钾
glaucoma [] 青光眼 retardation []
延迟
electrolytic [] 电 解 质 的 hypokinemia
[] 低血钾
osteoporosis [] 骨质疏松症
27
Chapter 26
Agents
Affecting the Thyroid
Gland
Anti thyroid agents
1 thioureas: used to treat mild or moderate hyperthyroidism, prior to the surgical
treatment of hyperthyroidis, as an adjuvant in thyroid crisis.
2 iodine/iodile: used for preoperative preparation; large doses for thyroid crisis:
3 radioactive iodine
4 β-blocking agents: many of the symptoms of thyrotoxicosis mimic those associated
with sympathetic stimulation, β-adrenoceptive blocking agents such as propranolol,
alprenold inhibit the conversion of peripheral T4 to T3 .
Thyroid [] 甲状腺
thiourea [] 硫脲基
Hyperthyroidism [] 甲状腺机能亢进
Adjuvant [] 辅佐的 iodine [;] 碘
Thyrotoxicosis [] 甲状腺功能亢进
28
Chapter 27
Antidiabetic drugs
Introduction : Diabetes mellitus is a common chronic disease, which is recognised
world-wide as a major public health problem. It is associated with markedly increased
morbidity and mortality, representing the fourth leading cause of death in
industrialised nations.
1 isulin
Uses: Type Ⅰan Ⅱ diabetes.
2 oral hypoglycemic agents
Sulonylureas: usde for type Ⅱ diabetes.
Biguanides
α-glucosidase inhibitors
repaglinide: a prandial glucose regulator for the treatment of type Ⅱ diabetes
morbidity [] 发病率 mortality[] 死亡率
hypoglycemic 低血糖症的 prandial [] 膳食的
29
Chapter 28
Antimicrobial Agents
1 concepts
Antibiotics: are substances produced by various species of microorganisms(bacteria,
fungi, actinomycetes) that suppress the growth of other microorganisms.
2 mechanism of antimicrobial agents
Inhibit the synthesis of the bacterial cell walls; act directly on the cell membrane of
the microorganism; affect of the function of 30S or 50S ribosomal subunits to cause a
reversible inhibition of protein synthesis; affect bacterial nucleic acid metabolism;
antimetabolites.
3 resistance to antimicrobial
30
Chapter 29 Beta-lactam antibiotics
1 penicillins
Penicillin G
Spectrum of activity: is effective against gram-positive cocci( pneumococci,
staphylococci, streptococci), gram-negative cocci( meningococci, gonococci),
gram-positive bacilli(bacillus perfringens, bacillus diphtheriae).
Mechanism: inhibit bacterial growth by interfering with a specific step in bacterial cell
wall synthesis.
Uses: used in the infections caused by the various susceptible G+ cocci.
Adverse reaction: allergic reaction.
Semisynthetic penicillins
Acid-resistant penicillins
Penicillinase-resistant penicillins: they are the drugs of first choice for treating
infections of the penicillinase-productive aurococcus.
Broad-spectrum penicillins
Antipseudomonal penicillins
2 Cephalosporins
Cephalosporins are similar to penicillins chemically, in mechanism of action, and
toxicity. Cephalosporins are more stable than penicillins to many bacterial
beta-lactamase and therefore ususlly have a broader spectrum of activity.
Spectrum of activity: cephalosporins can be classified into four major groups or
generations, depending mainly on the spectrum of antimicrobial activity.
31