Antibacterial Drugs

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					Antibacterial Drugs

Mohammed Almaskari
            Antibacterial Drugs
   Sulphonamide, Nitrofuranes
   Quinolones,      B lactams
   Chloraphenicol, Amino glycosides
   Miscellaneous antibiotics
   Main drugs used in tuberculosis
   Antibiotic drugs for common infections
             Pharmacodynamics
   Bacteriocidal        Bacteriostatic
-   Aminoglycosides   -   Sulphonamide
-   Penicillin        -   Tetracyclines
-   Cephalosporin     -   Urinary tract
-   Quinolones            antiseptics
-   Macrolides        -   Metronidazole
              Sulphonamide
   Sulfadimidine, silver sulfadiazine
   Treat UTI, ulcerative colitis,
    rheumatoid arthritis
   SE: Nausea, rash, fever
                     Nitrofuranes
   Nitrofurantoin
   Treat UTI
   SE: Nausea, rash, fever
   Not to give renal failure pt
                  Quinolones
   Ciprofloxacin, norfloxacin
   Treat UTI, gonorrhea, meningitis
   SE: GI upset, rash
   Avoid in epilepsy, children
                    B lactams
   Penicillin, cephalosporin, imipenem
   Tonsillitis, pneumonia, septicemia
   SE: allergy, diarrhea, pain
                Amino glycosides
   Amikacin, gentamicin
   Treat septicemia, pneumonia, chest infection,
    meningitis, TB (streptomycin)
   SE: ototoxicity, nephrotoxicity,rash, vomiting
   Avoid in renal function
                Chloraphenicol
   Uses in menengitis, epiglottitis, typhoid,
    eye & ear drops
   SE: rare- bone marrow depression,
    collapse & shock in newborn
     Miscellaneous antibiotics
   Vancomycin, clindamycin
   Treat colon, bone infection, peritonitis
   SE: ototoxicity, nephrotoxicity, diarrhea
   Caution: pregnancy, renal impairment
      Main drugs used in tuberculosis

   Isoniazid, rifampicin, ethambutol, streptomycin
   Bacteriostatic, ability to cross meningeal barrier
   SE: neuropathy, damage optic nerve, red secretion
   Avoid in liver disease
   Others
           Pharmacotherapeutics
   To treat gram-negative bacilli
   Nosocomial infection, UTI
   Infection of CNS
   Eye & ear infection
   Pneumococci
              Adverse Reactions
   Severe allergic reaction
   Altered in immunity
   Disturbed of normal bacteria activity in
    the body
   Antibiotic resistance organisms
Chapter 8
drugs affecting alimentary canal

          Silvia clement
Causes of delayed passage
   Local lesions
   Disorders of muscle function
   Pregnancy
   Old age
   Depression
   Weakness of the abdominal muscle
   Low bulk
   Drugs
Neglect of call to stool
   Pts who are ill and who constipated for
    few days two or four senokot tablets at
    night followed by glycerin suppository.
   For chronic constipation re-educate and
    bowel retraining. (fiber and fluid)
    brans,senokot
 Old age : exercise ,retention enema if
  still removel of impacted stool.
Senna and bisacodyl may be given.
Enemas and suppositories
 Enemas help to soften stools
 Phosphate enema is the common one
 Given before any major surgery or
 diagnostic procedures
 Enemas also used for other treatments
 like retention, irrigation (steroid enema
 in ulcerative colitis.)
    Suppositories
Glycerol suppositories one or two moistened with
  water and are inserted it is effective.
                 Intestinal sedatives
Several drugs may diminish the peristaltic activity
  of the intestines.
                Anticholinergic drugs:
Anticholinergic drugs decrease gut tone by
  blocking the action of parasympathetic nervous
  system also useful in colonal spasm.
Opioids
Opioids actually increase gut tone but
  reduce peristalisis
They are useful in various forms of diarhoea
Most commonly used is codine phosphate.
Co- phenotrope (lomotil) is combination of
  atropine diphenoxylate hydrochloride.
this is a narcotic and is widely used for
  diarhoea . Dangerous in overdose.
Drugs for diarrhoea
Lopramide :
Decreases large bowel motility
Toxicity is relatively low
Available as over the counter drug.
Pancreatic supplements
As a result of pancreatic disease (cystic
  fibrosis, and chronic pancreatitis).
Pancreatic enzyme is deficient so failure
  to digest fat and protein. (steatorrhoea)
Missing enzymes are given orally but
  broken in acid so combined with
  H2receptor antogonist or entric coated
  tablets.
Pancreatic supplements
1. Pancrex: given as powder, capsules,
   tablets.before meals should be mixed
   with water or milk.
2. Creon: capsules containing coated

   pellets that may be swallowed as
   wholeor mixed with food.
Should not chew.
Gall stones
Usually surgically removed
There are however drugs to dissolve gall
  stones.
Chenodeoxycholic acid and
Ursodeoxycholic acid.
Gall stones are largely composed of
  cholesterol.
These two drugs are bile salts.
Gall stones
1.   Only small stones are suitable for
     treatment.
2.   Two drugs are given together orally as
     single dose at bedtime.
3.   It may take 6-18 months to dissolve
     the stones to disappear.
Drugs and liver
   All drug pass through first pass
    metabolism.
   Many drugs are activated or inactivated
    by liver so liver disease affect activation
    or inactivation causing toxicity.
   Some drugs cause liver damage.
   Drugs are used to treat certain diseases
    of liver.
Drugs cause liver damage
1.   Paracetamol
2.   Phenothiazines
3.   Methotrexate
4.   Isoniazid
5.   Rifampicin
6.   Pyrazinamide
7.   Halothane
Chronic viral hepatitis
   Viral hepatitis B and C are serious health
    hazard
   Most of the time the diseases resolve by itself
    completely
   But 5% of infections continues and become
    chronic hepatitis
   Some patients re4main asymptomatic and
    become carriers of the virus
   Some develop cirrhosis and a few hepatic
    carcinomas.
Interferons
Only treatment available
These are peptides that are produced by
  the virus
Drug stimulate immunity and have
  antiviral action.
Active against wide variety of viruses.
50% hepatitis B and 25% hepatitis C The
  progress is halted.
Adverse effects
 Depression
 Flu like symptoms

 Lethargy

Vaccine are available plus specific
  hepatitis B immunoglobulin is also
  available when rapid protection is
  required.
A combined A and B vaccine is also
  available.
laxatives

                   By
            Silvia Clement.



4/2/2011
Adverse effects
    Nausea
   Shortness of breath
   Chest pain
   Flu like symptoms
   Contraindicated for TB



4/2/2011
PURGES IN TREATMENT OF CONSTIPATION
Purges or purgatives are drugs that loosen
  the bowel .
They are also called as cathartics or
  laxatives.
Bowel evacuation may be achieved using
  orally administered using orally
  administered purges or by the use of
  enemas and suppositories.

    4/2/2011
PURGES IN TREATMENT OF CONSTIPATION
 Purgatives may work in different ways and
   there are several types.
   Bulk purges –high residue foods eg bran.
   ispaghula husk
   Stool softners e.g docusate sodium
   Osmatic purges e.g magnesium
   sulphate,lactulose
   Stimulant purges e.g
   anthracenes,bisacodyl
    4/2/2011
   Bulk purges
High residue foods contain high proportion
  of cellulose which is not digested and thus
  not absorbed increases the bulk of the
  intestinal contents. eg wholemeal bread
Bran :by product of mills
Methyl cellulose :Is available in number of
 preparations. either as tablet or granules.

   4/2/2011
Bulk purges
Ispaghula husk: is a plant origin and
  swells on contact with water thus acting
  as bulk purge (Isogel and Regulan)
Bulk purges depend on the ability of the
 colon to respond to distenstion.may not
 be effective in elderly.


4/2/2011
   Stool softeners elderly who have
Liquid paraffin: used for
  chronic constipation.
It is odourless,tasteless and facilitates
  evacuation in chronic pts.
Adverse effects  (long term side effects)
 Leaking via anal sphinter

 Lipoid pneumonia in young and very old

 Interference with absorption of vit A ,D,K

 So it should not be used for long periods.


   4/2/2011
Osmatic purges
Saline purges:megnesium sulphate (epsom
  salts).
It is poorly absorbed from intestinal tract
Given in empty stomach.
Lactolose: is a sugar that is broken down by
  bacteria in large bowel with the
  production of various acids.
These acts as osmatic purges rendering the
  bowel contents more fluids and as mild
  irritants both of which produce a laxative
  effect.
    4/2/2011
The Stimulant purges
     athracene group of purges all contain
  the anthraquinone emodin, which is the
  chief active constituent of the group.
After liberation in the intestine emodin is
  absorbed into the blood stream and act on
  large intestine causing increased
  peristalsis.
All members of this group there fore take 8-
  12hours to act and so given at bed time

   4/2/2011
Stimulant purges
   Senna (senokot) granules are tablet.
   Bisacodyl- oral,suppository.
   Co-danthramer –given to terminally ill
    pt but rare.
   Sodium picosulfate –powerful stimulant
    used before surgery or radiological
    procedures.

4/2/2011
Laxative abuse
Adverse effects:
 Diarrhea with loss of fluids and
     elcrolytes
 Dependence on purges with chronic use

 Systemic absorption of purges

 Lipoid pneumonia with liquid paraffin

 Damage to bowel

 Abdominal pain
4/2/2011
Drugs used in chronic
    inflammatory
        disease

  Silvia clement
    Chapter 8
   Page no 115
Chronic inflammatory disease
Is an inflammation of the bowel and

includes Crohn’s disease and ulcerative

colitis.

These are chronic autoimmune diseases, In

which the immune system attacks the
DRUGS USED IN CIBD
Corticosteroids


Sulfasalazine


Mesaalazine


Immunosuppressant's


Infliximab
CORTICOSTEROIDS
   Used to induce remission in both
    disorders.

   Prednisolone is given orally until disease
    subsides then it is reduce stepwise.

   Budenoside (entocort) is a retarded
    release steroid that may have a more
    marked local action in the terminal small
 Sulfasalazine
After treatment with corticosteroid

sulfasalazine is then started to keep the pt in

remission .

Sulfasalazine is combination of 5 –amino

salicylic acid and sulfapyridine and is broken
      Sulfasalazine
Adverse effects :
   Headache ,Nausea
   Rashes, blood disorders
   Male infertility

Mesalazine: 5-amino salisalic acid has few
side effects than sulfazalizaline .
More expensive , enemas are give for distal
disease
Immunosuppresent’s
   Reduce the activity of immune system

   Reduce inflammation by inhibiting the
    production of immune cells or
    /interfering with their production of
    inflammatory proteins.

   This weaken the immune system and
    prone for infection.
Immunosuppresent’s
Azathioprine : is also used in
rheumatoid arthritis combined with
steroid so reduced dose of steroid is
given.
Methotrexate : used for cancer now
widely used to treat autoimmune
diseases
Immunosuppresent’s
Infliximab: (Remicade) Newer drugs
called biologics that block the action of
powerful immuno reactive chemicals that are
produced by the cells of immune system.
Widely used to treat autoimmune disease
Mechanism of action :
Infliximab binds to and inactivates an
important inflammatory protien of the immune
system called tumor necrosis factor (TN-α),
Infliximab: (Remicade)
 given as IV as in patient repeated
after 3 months to prevent relapse.
Effects : beneficial effect on Crohn's
disease can be very rapid and
dramatic for who does not respond to
other treatment
This drug is useful in healing anal
fistula of crohns disease
Adverse effects
   Nausea
   Shortness of breath
   Chest pain
   Flu like symptoms
   Contraindicated for TB
PURGES IN TREATMENT OF
CONSTIPATION
  Purges or purgatives are drugs that

   loosen the bowel .

  They are also called as cathartics or

   laxatives.
PURGES IN TREATMENT OF
CONSTIPATION
  Purgatives may work in different ways
   and there are several types.
   Bulk purges –high residue foods eg
   bran. ispaghula husk
   Stool softners e.g docusate sodium
   Osmatic purges e.g magnesium
             Bulk purges
High residue foods contain high
  proportion of cellulose which is not
  digested and thus not absorbed
  increases the bulk of the intestinal
  contents. eg wholemeal bread
Bran :by product of mills
Methyl cellulose :Is available in number of
           Bulk purges

 Ispaghula husk: is a plant origin and

swells on contact with water thus acting

   as bulk purge (Isogel and Regulan)

Bulk purges depend on the ability of the

 colon to respond to distenstion.may not
Stool softeners
Liquid paraffin: used for elderly who have
  chronic constipation.
It is odourless,tasteless and facilitates
  evacuation in chronic pts.
Adverse effects  (long term side effects)
 Leaking via anal sphinter

 Lipoid pneumonia in young and very old

 Interference with absorption of vit A
  ,D,K
Osmatic purges
Saline purges:megnesium sulphate (epsom
  salts).
It is poorly absorbed from intestinal tract
Given in empty stomach.
Lactolose: is a sugar that is broken down by
  bacteria in large bowel with the production of
  various acids.
                 Stimulant purges
The athracene group of purges all contain the anthraquinone
  emodin, which is the chief active constituent of the group.
After liberation in the intestine emodin is absorbed into the
  blood stream and act on large intestine causing increased
  peristalsis.
All members of this group there fore take 8-12hours to act
  and so given at bed time
         Stimulant purges

   Senna (senokot) granules are tablet.

   Bisacodyl- oral,suppository.

   Co-danthramer –given to terminally ill

    pt but rare.
            Laxative abuse
Adverse effects:
   Diarrhea with loss of fluids and elcrolytes
   Dependence on purges with chronic use
   Systemic absorption of purges
   Lipoid pneumonia with liquid paraffin
   Damage to bowel
   Abdominal pain
Anesthetic Agents &
Drugs used during CPR
       Mohammed Almaskari
     Anesthesia
   Inhalational anesthesia
   Opioid analgesic
   Muscle relaxants
   Ant cholinergic drugs
   Local anesthesia
    Inhalational Anesthesia
 Nitrous oxide (laughing gas)
 Halothane

 Some have analgesic effects

 Sevoflurane is used in children

Local anesthesia:
 Lidocaine, bupivacaine, cocaine
Opioid Analgesic
   Morphine, fentanyl
   Analgesic, sedatives, respiratory
    depression
   Naloxone is Antidots
Muscle Relaxants
   Atracurium, vecuronium
   Used to facilitate intubations, doing
    surgery, & permit artificial ventilation
   Anticholinesterase is the Antidots
   Anticholenergic to reduce the side effects
     Anti cholinergic drugs
   Atropine
   Increase pulse rate
   Reduce bronchial secretion
   Reduce peristalsis movement
Drugs used during CPR
   ABC during CPR
   O2, ECG, IV access
   Adrenaline
   Amiodarone
   Lidocaine
   Adenosine Na+ bicarbonate
   Atropine
Antidepressants & Dementias

      Mohammed Almaskari
     Depression
   Psychological causes (mania)
   Reduction in the serotonin
-   Tricyclic antidepressants
-   Tricyclic anxiolytics
-   Lithium
-   SSRIs, MAOIs, others
Tricyclic Antidepressants
   Amytriptline, imipramine
   Treat sleep disorders, facial pain,
    bedwetting
   The effect may take 2-6 weeks
   SE: dry mouth, postural hypotension,
    increase appetite, cardiac toxic
   Overdose, withdrawal symptoms
     Tricyclic anxiolytics
   Doxepin, maprotiline
   Treat anxiety-lead mild depression
   SE: cardiotoxic
    Trazodone (for cardiac pt)
Lithium
   Treat polar & manic depression
   Haloperidol for acute mania
     Dementia
   Alzheimer, strokes
   Donepezil, galantamine
   Combination of antdepressants,
    anxiolytics, antipsychotic
   Health Education (P. 287)
Drugs affecting the alimentary
tract

               Silvia clement
                 Cs -15-16
                Page no108

2 April 2011
Learning objectives
   List the treatment for acid reflux and
    describe how acid and pepsin are
    produced.
   Discuss the antacids and the problems
    associated with their use.




     2 April 2011
List of drugs in acid reflux
disease
Gaviscon and gastrocote are combination
of an antacid with alginates which floats
on gastric contents and at reflux they
protect the mucosa.
Mucaine: contains the antacids aluminum
hydroxide and magnesium hydroxide with
oxeticane local anesthetic which relieves
pain reduces gastric acidity.
Histamine H receptor blockers: reduce
           2
2 April 2011
List of drugs in acid reflux
disease
   Proton pump inhibitors: abolish acid
    secretion completely and are more
    effective used in severe disease of
    esophageal reflux disease.
 Metoclopramide :stimulates
    oesophageal motility and thus keeps
    the oesophasus empty and is useful
 Domperidone : same like
    metaclopamide
2 April 2011
Production of acid and pepsin
Is a complex process there are two ways
1. Stimulation of vagus nerve leads to
   secretion of acetylcholine intern increases
   acid secretion.
2. Distension of the stomach causes the

   production of hormone gastrin and this in
   turn stimulates the stomach to produce
   acid.

    2 April 2011
Production of acid and pepsin
               Histaminocytes.

                 Histamines

                proton pump

                parietal cells
2 April 2011
Treatment of peptic ulcers and
dyspepsia

Aims of treatment :
   To reduce acidity which relieves pain and
    also helps the healing process.
   To protect the ulcer from further damage
    by acid.
   To eradicate H. pylori infection
   To discourage the use of NSAIDS


     2 April 2011
DRUGS FOR REDUCING ACIDITY

     Antacids
     Histamine H2 receptor blockers
     Proton pump inhibitors.
     Tripotassium dicitratobismuthate
      chelate
     Sucralfate
     Prostoglandins -mesoprostol
  2 April 2011
Antacids

  Widely used in treatment of peptic ulcers
      and other forms of dyspepsia
    act by reducing the acidity in stomach
      and they also reduce pepsin activity
  Temporarily Reduce pain of ulcer
  Magnesium trisilicate white gritty
      powder usually prescribed as prescribed
      as a mixture that contains sodium
      hydrogen carbonate and magnesium
      carbonate.
  2 April 2011
Antacids

  Aluminum hydroxide:
  White powder insoluble in water and
      usually given as a mixture or a tablet
  Tablets are sucked to prolong the action
  In addition to reduce acidity aluminium
      salts inactivate gastric pepsin
  It is slightly astringent and shrink cells –
      cause constipation
  Frequency of dosage is important given 1
  2 April 2011
      hr aftermeals.
        BLOCKING GASTRIC ACID
        SECRETION
 Gastric acid secretion is reduced in two
  ways.
1. By blocking the action of histamine at H2
   receptor
2. By inhibiting proton pump

 Histamine receptor H2 blockers
       Ranitidine
       Cimetidine
       Famotidine
       nizatidinie
        2 April 2011
     Histamine H2 blockers
    block the action of histamine on the
    receptor in the stomach wall (reduce acid
    70%)
   Given as oral and injection form
   Ulcer s/s disappear within a week 85%
    duodenal ulcers heal
   Gastric ulcer take long time
   Once the drug is stopped recurrence is
    common
             in
    Used 2011 reflux esophagitis
      2 April
Adverse effects
  rare with cimetidine gynacomastia
Male impotence
Confusion in elderly.
             Proton pump inhibitors
Lasoprasol
Omeprazol
Pantoprazol
These drugs inhabit gastric acid secretion
2 April 2011
Proton pump inhibitors
 Used to treat peptic ulcers who does
  not respond to H2 Receptor
 Combined with antibiotics to eliminate

  H pylori.
 Used in reflux esophagitis

 Zollinger ellison syndrome

Adverse effects:
         Headache
2 April 2011
      Nausea,diarrhoea,rashes
     Ulcer protection
   Tripotassium dictratobismuthate chelate
Contains bismuth compound and causes
coagulation at the base of ulcer protecting it.
Unpleasant taste
Tongue and stool appear black
Treatment continued for 4 weeks
 Sucralfate:compound of aluminium and
  sucrose that coats the base of an ulcer
  protecting it and healing take place.
    2 April 2011
Ulcer protection
 Prostaglandins e.g misoprostol
Prostoglandins exert some protective
effect on the gastric mucosa.
Misoprostol has shown to reduce risk of
gastric ulcer



2 April 2011
    Eradication of h pylori
 Omeproazole+metronidazole+amoxicillin
1 week effective and cheap
 Omeproazole+clarithromycin+metronidazole

1 week
 Omeproazole+clarithromycin+amoxicillin

1week
 Ranitidine +amoxicillin+metronidazole

2 weeks
    2 April 2011
Emitics, antiemitics cough
remedies and respiratory
Stimulats
          Silvia clement
Learning objectives
1.   Give an account of the emetics and
     classes of antiemetic drugs.
2.   Understand the uses and limitations of
     cough suppressants.
3.   Describe inhalations and mucolytic
     agents.
Central emetics
(those act on brain)

            ctz




          Vomiting
           center
Central emetics
   Apo morphine : stimulates dopamine
    receptors in the CTZ.
   It is closely related to morphine has
    none of its analgesic properties.
   It was formally an emetic but because
    of its depressant action it should not be
    given to pts who are in overdose.
    Central emetics
 It is believed that acetylcholine ,histamine

    ,dopamine and 5 HT act as intermediate
    transmitters in the CTZ and vomiting
    center.
   By blocking the action of these substances
    on their receptors .
   It is possible to prevent or diminish
    vomiting.
Classification of antiemetics
 Acetylcholine receptor antagonists.
 Antihistamines
 Dopamine receptor antagonists
 5-HT receptor antagonists
 Miscellaneous antiemetics
Muscarinic acetylcholine
receptor antagonists
   Hysocine blocks the action of
    acetylcholine on the vomiting center
   Is useful for short term control of
    motion sickness
   It is administered as trans dermal patch
   Behind the ear 6 hours before starting
    the journey.
    Anti histamines
Anti histamines are commonly used as anti
emitics.
1. Cyclizine

2. Promethazine

3. Cinnarizine

Anti histamines are not specific and also
block Ach receptors .this makes them
effective antiemetics.
Anti histamines
Cyclizine and promethazine used for
severe vomiting in pregnancy
Cinnarizine is an antiemetic for yatchmen
And menieres disease.
    Dopamine antogonists
 Phenothiazine are powerful antiemitics

   Due to their action of blocking the effects
    of dopamine on the CTZ.
   They are non specific and have side
    effects.(sedatives)
   Prochlorperazine
   Chlorpromazine
   Domperidone
   metaclopramide
Prochlorperazine
   Suppress opioid induced vomiting
   It can be given orally or intramuscular
    but not subcutaneous.
   If given intravenous it should be well
    diluted.
   Chlorpromazine is similar to
    prochlorperazine.
    Domperidone
 Less sedative

   Its action is confined to CTZ of nervous
    system
   It also enhances gastric emptying
   Only 15 % of drug reaches circulation and
    parentral preparation is not available.
   Used to suppress opioid induced ,levodopa
    cytotoxic drug induced in long term
    treatment .
Metaclopramide
   Increases the gastric tone and dilates
    the duodenum
   This causes the stomach to empty
    faster
   In addition it has action on the vomiting
    centre .
   Fairly effective anti emetic
   Administered orally and intravenous
   Given post op and migrane
Metaclopramide
   Adverse effects are rare
   Pt may develop dystonia of facial and
    neck muscles
5 HT antogonists
Ondansetron and granisetron probably
block the 5 HT receptors associated with
central connections of vogues nerve in
brain stem.
   Cough remedies
Expectorants: expectorants are drugs that
loosen the sputum and thus aid its ejection
from the bronchial tree.
Many drugs are available over the counter.
Cough suppressants (antitussive) drugs.
Under certain circumstances it is
advantageous to suppress a cough that is
tiring pt and serving no useful purpose.
Cough suppressants (antitussive) drugs
   This can lead to sputum retention and
    thickening.
   Antitussive should not be given to pt with
    chronic bronchitis ,bronchiectasis or cough
    associated with asthma.
Demulcents : cough arising from irritation
of mucus membrane, may be suppressed
through smoothening action of syrup.
Which forms a protective layer over
inflamed tissue (not given for DM pts)
    Opioids depressant drugs morphine
 Effective cough

    codine,heroin.
   These drugs are present in many cough
    syrups and an effective antitussive.
Codeine: most popular included in
linctus codeine. pholcodiene is closely
related to this drug action is 4-6hs
Very effective if given over dose may
constipate.
    Dexamethorphan
 Is a synthetic narcotic analgesics
 Many over the counter drugs are available

 it is as potent as codeine in cough

  suppressant.
 Can cause constipation

Inhalations and mucolytic; benzoin tincture
one of balsams contain resins and volatile
oils. added to hot water
Pulmonary surfactant
   In premature babies the factor is
    lacking
   This is treated with synthetic surfactant
    inhalations like colfosceril palmite
Respiratory stimulant (doxapram)
Most effective respiratory
stimulant given by intravenous
Anti- Inflammatory Drugs
      Mohammed Almaskari
     Objectives
   To know the NSAIDs and its actions
   To understand the different use of NSAIDs
   To list the main drugs that are used in
    Rheumatoid disease and gout.
      NSAIDs
   Salicylates (Aspirin, ponestan)
   Analgesic, anti-inflammatory, antipyretic.
   Rheumatoid arthritis & fever
   SE: gastric irritants, bleeding
   Aspirin poisoning
     NSAIDs
   Paracetamol
   Analgesic, antipyretic.
   Prefer for children
   Liver & renal problems in overdose
       NSAIDs
   Non-selective Cox NSAIDs
   Diclofenac, Ibuprofen
   Analgesic, antipyretic.
   SE: gastric bleeding, edema, bronchospasm
Rheumatoid Arthritis
   Aim: to prevent deformity & control pain,
    swelling, stiffness of the joints
   NSAIDs, SAIDs, DMARDs
   DMARDs (chloroquine) inhibits effect of
    immune system on RA.
   SE: vision disturbance
     Gout
   Colchicine
   Uricosuric (sulfinpyrazone)
   Allopurinol
Anti- Viral & Antifungal Drugs


     Mohammed Almaskari
                   Antifungal

   Nystatin, miconazole, metronidazole
   Bind to fungus wall & destruct it
   Treat candidiasis, skin & lung infection
   Page 333
Drugs used in atheroma and
angina

          Chapter 7
        Silvia clement
       30 October 2010
Atheroma and arterial thrombosis

   An Atheroma is a mass or plaque of
    fatty or tissue on the inner lining
    (intima) of arterial wall that occurs due
    to damage and degeneration of the
    intima
Atheroma and arterial thrombosis
CAUSES OF ATHEROMA :
  1.   Stress and strain due to raised blood

       pressure

  2.   High levels of cholesterol

  3.   Irritants and tobacco
Atheroma and arterial thrombosis

   The coronary arteries causing ischemic heart

    disease

   The carotid and cerebral arteries causing strokes.

   The leg causing claudication which is limping or

    lameness
Ischemic heart disease
  Risk factors ,age increased BP ,smoking
            increased cholesterol


     Atheroma in blood vessels


      Effort angina ,chest pain (if thrombus
   blocks blood
 vessel )

           Myocardial infarction
Drugs used in angina effort
Several group of drugs relieve the symptoms of
  angina but they do not reverse the underlying
  Atheroma.
The nitrates :
 Glyceryl trinitrate

 Isosorbide dinitrate

 Isosorbide mononitrate

 Beta blockers

 Calcium antagonists
The nitrates
These drugs act directly on the plain muscle of
   the body causing it to relax in the walls of
   blood vessels.it relieve pain of angina in two
   ways
  1.   By vasodilatation reduces venous return
       reduces the heart work reduces demand of
       oxygen.

  2.   By dilating the coronary arteries particularly if in
       spasm ,so that the blood flow through these
Glyceryl trinitrate
Glyceryl trinitrate :
              Is an oily liquid .it is prepared as
    tablets by mixing with an absorbent base
 it is also prepared as metered aerosol impregnated
    skin patches or IV infusions.
Tablets:
sublingually ,or as whole ,first pass metabolism.
    Last 15-20 min
Should not be kept more than 2 months
Store in dark glass container not exposed to light
    ,cotton wool
Glyceryl trinitrate
Metered aerosol: a very useful alternative is to
 give glycerol trinitrate via is metered aerosol

Acts rapidly it is sprayed under tongue and the
  mouth is then cleaned .

Skin patches : absorbed through skin acts 24hrs
Difficult to control dosage head ache is common
  side effect.
Glyceryl trinitrate
IV infusion used to reverse for pt with
    severe chest pain usually following MI.
    mixed with 5% Dextrose or 0.9 NS By
    infusion pump.
Effects :
     1.   General vasodilatation
     2.   Fall in blood pressure.
Isosorbide dinitrate and
mononitrate
Isosorbide dinitrate : Is similar to
   trinitrate
        broken down in liver.
Isosorbide mononitrate:
  1.   Active agent
  2.   Available for clinical use
  3.   Given twice daily
  4.   Action is quite prolonged
  5.   Mono and dinitrate is available in IV form
Clinical use of nitrates
1.   Treatment of angina effort.
2.   May be taken intermittently to relive pain
     in an attack.
3.   Taken before any activity Glyceryl
     trinitrate is the best drug for this
     purpose.
4.   One tablet sublingual is sucked under
     tongue dose may be repeated
     frequently.
5.   Long acting sustained release dinitrate or
     mononitrate can be given regularly to
Adverse effects
1.   Flushing
2.   Headache
3.   Palpitations
4.   A fall in BP which can cause fainting
     attacks in long acting preparations.
Tolerance
   Tolerated well
   IV infusions should not be given more
    than 36 hrs without break.
   Sustained release or long acting prep
    should be taken along with evening
    meal
   Skin patch is removed unless if pt has
    nocturnal angina
Calcium antogonists
Are potent vasodilators
     1.   Nifedipine
     2.   Verapamil
     3.   Diltiazem
     –    All are used to treat angina decrease the
          work load of heart by dilating peripheral
          blood vessels.
     –    In addition coronary vasodilatation.
     –    In CAD pt short acting Nifedipine are not
          used.
     –    These are taken regularly.
     –    Slow release Nifedipine (adalat) given
          twice daily
     –    Verapamil &Diltiazem three timely
Adverse effects
1.  Headache
2.  Flushing
3. Nausea.
Unstable angina
   Occurs irregularly and attacks at rest
   This indicates a detached Atheroma can
    cause MI.
   Low dose of aspirin is used to prevent
    formation of clot
   Glyceryl trinitrate relieves pain
   Beta blockers are give at first to reduce
    the risk of MI
   Heparin should be used should not be
    delayed
Patient education
   Avoid stress
   Should know the different types of
    treatment ( in acute attack, prevention)
   Should be familiar with side effects
   Explain to pt that if taken continuously it is
    unlikely to happen the reduction in effect
    with Glyceryl trinitrate.
   To call the doctor if drugs does not
    respond and the attack is prolonged
   Avoid all risk factors.
                Antibaviral Drugs
   Virus can survive & multiply rapidly
   Aciclovir, Ganciclovir, amantadine
   inhibit virus DNA polymerase & replication.
   Treat cold sore, influenza, chickenpox,
    mumps, herpes simplex
   SE: suppress WBC, platelets
.
                 The Interferons
   Adefovir, entecavir
   Protein-like substance produced in reaction
    to virus.
   Have ability to increase cell resistance to
    viral infections
   Treat hepatitis B & C
laxatives

                   By
            Silvia Clement.



4/2/2011
Adverse effects
    Nausea
   Shortness of breath
   Chest pain
   Flu like symptoms
   Contraindicated for TB



4/2/2011
PURGES IN TREATMENT OF CONSTIPATION
Purges or purgatives are drugs that loosen
  the bowel .
They are also called as cathartics or
  laxatives.
Bowel evacuation may be achieved using
  orally administered using orally
  administered purges or by the use of
  enemas and suppositories.

    4/2/2011
PURGES IN TREATMENT OF CONSTIPATION
 Purgatives may work in different ways and
   there are several types.
   Bulk purges –high residue foods eg bran.
   ispaghula husk
   Stool softners e.g docusate sodium
   Osmatic purges e.g magnesium
   sulphate,lactulose
   Stimulant purges e.g
   anthracenes,bisacodyl
    4/2/2011
   Bulk purges
High residue foods contain high proportion
  of cellulose which is not digested and thus
  not absorbed increases the bulk of the
  intestinal contents. eg wholemeal bread
Bran :by product of mills
Methyl cellulose :Is available in number of
 preparations. either as tablet or granules.

   4/2/2011
Bulk purges
Ispaghula husk: is a plant origin and
  swells on contact with water thus acting
  as bulk purge (Isogel and Regulan)
Bulk purges depend on the ability of the
 colon to respond to distenstion.may not
 be effective in elderly.


4/2/2011
   Stool softeners elderly who have
Liquid paraffin: used for
  chronic constipation.
It is odourless,tasteless and facilitates
  evacuation in chronic pts.
Adverse effects  (long term side effects)
 Leaking via anal sphinter

 Lipoid pneumonia in young and very old

 Interference with absorption of vit A ,D,K

 So it should not be used for long periods.


   4/2/2011
Osmatic purges
Saline purges:megnesium sulphate (epsom
  salts).
It is poorly absorbed from intestinal tract
Given in empty stomach.
Lactolose: is a sugar that is broken down by
  bacteria in large bowel with the
  production of various acids.
These acts as osmatic purges rendering the
  bowel contents more fluids and as mild
  irritants both of which produce a laxative
  effect.
    4/2/2011
The Stimulant purges
     athracene group of purges all contain
  the anthraquinone emodin, which is the
  chief active constituent of the group.
After liberation in the intestine emodin is
  absorbed into the blood stream and act on
  large intestine causing increased
  peristalsis.
All members of this group there fore take 8-
  12hours to act and so given at bed time

   4/2/2011
Stimulant purges
   Senna (senokot) granules are tablet.
   Bisacodyl- oral,suppository.
   Co-danthramer –given to terminally ill
    pt but rare.
   Sodium picosulfate –powerful stimulant
    used before surgery or radiological
    procedures.

4/2/2011
Laxative abuse
Adverse effects:
 Diarrhea with loss of fluids and
     elcrolytes
 Dependence on purges with chronic use

 Systemic absorption of purges

 Lipoid pneumonia with liquid paraffin

 Damage to bowel

 Abdominal pain
4/2/2011

				
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