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LA blocks generation & conduction of nerve impulse at all parts of neuron where they come in contact, without
causing any structural damage. Thus, not only sensory but also motor impulses are interrupted when LA is applied to
mixed nerve, resulting in musclular paralysis & loss of autonomic control as well.
Classification:-
(ii) Insoluble
Benzocaine
Oxethazaine
Mechanism of action :-
Concentration of LA increases
Slowing of conduction
Conducation block
GAs are drugs which produce reversible loss of all sensation & conciousness.
Classification:-
Dissociative :- Catemine
1. Sedatives :- are the drugs which reduces excitement, calms the subject without producing sleep, though
drowsiness can be produced. Commonly used as Anxiolytics.
2. Hypnotics :- are th drugs which induce or maintain sleep similar to normal arousable sleep.
Sedatives & Hypnotics both are CNS depressants with somewhat differing time action & dose relationship.
Classification:-
(ii) Anti-anxiety
Diazepam
Alprazolam
Oxazepam
Lorazepam
(iii) Anti-convulsant
Zopiclone
Zolpidem
Zaleplon
Tranquilizer :- is an old term meanins ‘A drug which reduces mental tension & produces calmness without inducing
sleep or depressing mental faculties.’ E.g, benzodiazepines.
ANTIPYRETICS :- are the drugs which reduce body temperature in fever but do not cause hypothermia in
normothermic individulas.
ANALGESICS :- are the drugs which relieve pain without causing loss of conciousness.
Classification:-
(i) As analgesic for headache, backache, myaglia, joint pain, pulled muscle, toothache, dysmenorrhoea.
(ii) As antipyretic It is efffective in fever of any origin; dose same as analgesics. Anti-pyretics are not usefull in fever
due to heat stroke.
(iii) In Acute rheumatic fever
(iv) In Rheumatoid arthritis
(v) In Osteoartheritis
Mechanism of action :-
Antipyresis mechanism :- Fever during infection is produced through the generation of pyrogenes which induce
PGE2 (Prostaglandin E2, Also known as Dinoprostone ) production in hypothalamus – raise its temperature set point.
NSAIDs block the action of pyrogene & reduces body temperature.
Analgesia mechanism :- PGs induce hyperalgesia by affecting the transducing property of free nerve ending. NSAIDs
do not affect the tenderness induced by direct application of PGs, but block the pain sensitizing mechanism induced
by analgesic substances. So, they are more effective againts inflammation associated pain.
Side effects :-
Nausea
Vomiting
Epigastric distress
Increased occult blood loss in stool
Gastric mucosal damage
Peptic ulceration
Antiepilepticts are the drugs usefull in treatment of epilepsy. Epilepsy is a collective term for a group of chronic
seizures having common sudden and transient episodes of disterbance of consiousness and/or a charecteristic body
movement and sometimes autonomic hyperactivity.
Classification:-
1. Barbiturate Phenobarbitone
2. Deoxybarbiturate Primidone
3. Hydantoin Phenytoin
Fosphenytoin
4. Iminostilbene Carbamazepine
Oxcarbazepine
5. Succinimide Ethosuximide
7. Benzodiazepines Clonazepam
Diazepam
Lorazepam
Clobazam
8. Phenyltriazine Lamotrigine
Classification:-
(iii) K+ Sparing
Spironolactone
Amiloride
Antianginal drugs are those that prervent, abort or terminate attacks of angina pectoris.
Angina pectoris ls a pain syndrome due to indurction of an adverse oxygen supply / demand situation in a portion of
the myocardium.
Classification:-
2. β Blocker Propranolol
Metoprolol
Atenolol
(ii) Benzothiazepine :-
Diltiazem
(iii) Dihydropyridines :-
Nifedipine
Felodipine
Amlodipine
Nitrendipine
5. Others Dipyridamole
Trimetazidine
Ranolazine
Ivabradine
Oxyphedrine
ANTIPLATELET DRUGS :- These are drugs which interfere with platelet function and are useful in the prophylaxis
of thromboembolic disorders. E.g, Aspirin, Ticlopidine, Sulfinpyrazone, Clopidogrel.
These are drugs which lower the levels of lipids and lipoproteins in blood.
The hypolipidaemic drugs have attracted considerable attention because of their potential to prevent cardiovascular
disease by retarding the accelerated atherosclerosis in hyperlipidaemic individuals.
Classification:-
5. Others Ezetimibe
Gugulipid
HAEMOPOETICS :- are substances required in the formation of blood and are used for treatment of Anaemias.
COAGULANTS :- These are substances which promote coagulation and are indicated in haemorrhagic states.
Fresh whole blood or plasma provide all the factors needed for coagulation and are the best therapy for deficiency
of any clotting factor; also they act immediately. Other drugs used to restore haemostasis are :-
1. Vitamin K
K1 (from plants, fat-soluble)
K3 (synthetic) (i) Fat-soluble :- Menadione (ii)Water-soluble :- Menadione sod. Bisulfite
2. Miscellaneous
Fibrinogen (human), Antihaemophilic factor, Desmopressin, Adrenochrome monosemicarbazone, Rutin, Ethamsylate
Classification:-
1. β2 Sympathomietics Salbutamol
Terbutaline
β 2 receptor stimulation Bambuterol
Salmeterol
increased cAMP formation
Formoterol
in bronchial muscle cell
They are fastest acting bronchodilators when inhaled.
relaxation
They should be coutiously used in hypertensives & heart patients.
AEROSOLS / INHALANTS :- is a colloid system in which solid or liquid particles are suspended in a gas especially a
suspension of a drug or other substance to be dispensed in a fine spray or mist. E.g, ASTHALIN.
Four classes of antiasthma drugs are available for inhalational use, viz. β2 agonists, anticholinergics, cromoglycate
& glucocorticoids. They are aimed at delivering the drug to the site of action so that lower dose is needed &
systemic side effects are minimized. Faster action of bronchodilators can be achieved compared to oral
administration. Most asthma patients are now maintained on inhaled medication only.
Aerosols are of two types :- (i) use drug in solution :- pressurized metered dose inhaler (pMDI), nebulizers
(ii) use drug as dry powder :- spinhaler, rotahaler
These are drugs which increase bronchial secretion or reduce its viscosity, facilating its removal by coughing.
Classification:-
2. Mucolytics Bromhexine
Ambroxol
Acetyl cysteine
Carbocisteine
Sodium and potassium citrate are considered to increase bronchial secretion by salt action.
Potassium iodide is secreted by bronchial glands and can irritate the airway mucosa. Prolonged use can affect
thyroid function and produce iodism. It is not used now.
Guaiphenesin, vasaka, tolu balsum are plant products which are supposed to enhance bronchial secretion and
mucociliary function while being secreted by tracheobronchial glands.
Mucolytics
Bromhexine A derivative of the alkaloid vasicine obtained from Adhatoda vasica (Vasaka), is a potent mucolytic and
mucokinetic, capable of inducing thin copious bronchial secretion.
Dose:- adults 8mg TDS, children 1–5 years 4mg BD, 5–10 years 4mg TDS.
BROMHEXINE 8mg tablet, 4 mg/5 ml elixir.
Ambroxol A metabolite of bromhexine having similar mucolytic action, uses and side effects.
Dose:- 15–30mg TDS.
AMBRIL, AMBROLITE, AMBRODIL, MUCOLITE 30 mg tab, 30 mg/5ml liquid, 7.5mg/ml drops.
Acetylcysteine It opens disulfide bonds in mucoproteins present in sputum—makes it less viscid, but has to be
administered directly into the respiratory tract.
MUCOMIX 200mg/ml inj in 1,2,5 ml amps; injectable solution may be nebulized/instilled through trachiostomy tube.
Carbocisteine liquefies viscid sputum in the same way as acetylcysteine and is administered orally (250–750mg TDS).
MUCODYNE 375 mg cap, 250 mg/5 ml syr.
They are occasionally beneficial, only when elaboration of enzymes in G.I.T. is deficient. Their routine use in tonics
and appetite improving mixtures is irrational.
1. Pepsin May be used along with HCl in gastric achylia due to atrophic gastritis, gastric carcinoma, pernicious
anaemia, etc.
2. Papain It is a proteolytic enzyme obtained from raw papaya. Its efficacy after oral ingestion is doubtful.
3. Pancreatin It is a mixture of pancreatic enzymes obtained from hog and pig pancreas. It contains amylase, trypsin
and lipase.
4. Diastase and Takadiastase These are amylolytic enzymes obtained from the fungus Aspergillus oryzae.
Preparations:-
DIGEPLEX (Diastase 62.5 mg, pepsin 20 mg per 10 ml after dissolving the tablet in sorbitol base provided)
DIZEC (Pancreatin 250 mg, sod. Tauroglycocholate 50 mg, Methyl polysiloxane 25 mg tab.)
CARMINATIVES
These are drugs which promote the explusion of gases from the G.I.T. and give a feeling of warmth & comfort in the
epigastrium.
Sodium bicarbonate reacts with gastric HCL & envolves CO2 which rapidly distands stomach, relaxes LES & brings
about erructation.
The others are condiments and spices, contain volatile oil, which by their mild irritant action & flavour relax LES &
increase G.I.T. motility.
Peptic ulcer (especially duodenal) is a chronic remitting and relapsing disease lasting several years. The goals of
antiulcer therapy are :-
• Relief of pain
• Ulcer healing
• Prevention of complications (bleeding, perforation)
• Prevention of relapse.
Classification:-
(ii) Nonsystemic
Magnesium hydroxide
Aluminium hydroxide
Calcium carbonate
(a) Laxative or aperient :- milder action, elimination of soft but formed stools.
(b) Purgative or cathartic :- stronger action resulting in more fluid evacuation.
Many drugs in low doses act as laxative and in larger doses as purgative.
Classification:-
Psyllium & Ispaghula (ISOGEL- 27g./ 30g., FYBOGEL 3.5g./ 5.4g. powder)
AGAROL (liquid paraffin 9.5ml, phenophthalein 400mg, agar 60mg / 30ml emulsion)
Soft, formed faeces (take 1–3 days) Semifluid stools (take 6–8 hrs) Watery evacuation (take 6–8 hrs)
Bulk forming Phenolphthalein Saline purgatives
Docusates Bisacodyl Castor oil
Liquid paraffin Sod. Picosulfate
Lactulose Senna
Mechanism of action :-
(a) A hydrophilic or osmotic action, retaining water and electrolytes in the intestinal lumen—increase volume of
colonic content and make it easily propelled.
(b) Acting on intestinal mucosa, decrease net absorption of water and electrolyte; intestinal transit is enhanced
indirectly by the fluid bulk.
(c) Increasing propulsive activity as primary action—allowing less time for absorption of salt and water as a
secondary effect.
Purgative abuse :-
Some individuals are obsessed with using purgatives regularly. This may be the reflection of a psychological problem.
Others use a purgative casually, obtain thorough bowel evacuation, and by the time the colon fills up for a proper
motion (2–3 days) they get convinced that they are constipated and start taking the drug regularly. Chronic use of
purgatives must be discouraged. Once the purgative habit forms, it is difficult to break. Dangers of purgative abuse
are:
Diarrhoea is too frequent, often too precipitate passage of poorly formed stools. It is defined by WHO as 3 or more loose or
watery stools in a 24 hour period. In pathological terms, it occurs due to passage of excess water in faeces.This may be due to:-
Principles of management :-
3. Drug Therapy
Vomiting occurs due to stimulation of the emetic (vomiting) centre situated in the medulla oblongata. Multiple
pathways can elicit vomiting.
Classification:-
1. Anticholinergics Hyoscine
Dicyclomine
2. H1 antihistaminics Promethazine
Diphenhydramine
Dimenhydrinate
Doxylamine
Meclozine (Meclizine)
Cinnarizine
Ondansetron (EMSET, OSETRON, EMSETRON 4,8mg tabs.; 2mg/ml inj. In 2ml & 4ml amps.)
Granisetron (GRANICIP, GRANISET 1mg,2mg tabs; 1mg/ml inj. In 1ml & 3ml amps.)
These are the agents usefull for prevention & treatment of hepatic diseases.
Prevention :-
Treatments :-
Anti-hepatotoxic
Hepatotropic
Hepatoprotective
Usefull herbs :-
Marketed formulatons :-
LIV-52
LIMARIN
Diuretics are the drugs which increase the urine formation together with natriuresis. E.g, Furosemide, Thiazides
Only a few drugs produce diuresis by increasing GFR, and these are relatively weak in action. Most of the diuretics
used to therapeutically act by interfering with sodium re-absorption by the tubules.
Classification :-
Usefull in :-
Headache
Dizziness
Thirst
Gout
Diarrhoea
Skin rashes
Muscle cramps
Kidney failure
These are drugs that reduce urine volume particularly in diabetes insipidus.
Classification :-
3. Miscellaneous Indomethacin
Chlorpropamide
Carbamazepine
USES :-
Diabetes insipidus
Bedwetting in children & nocturia in adults
Renal concentration test
Haemophillia
Before abdominal radiography
LITHOTRIPTICS :- These are the drugs which break down the calculi either renal or ureteric.
In modern pharmacology there are no substances that have lithotriptic capebility & are harmless to the patients.
Shweta parpati
Palash kshara
Goksuradi guggulu
Pashanbheda churna