Pharmacology B

• chemotherapeutics: beta-lactam antibiotics: penicillins
• cell wall synthesis inhibitors

Narrow-spectrum type: for sensitive strains of streptococci, meningiococci and spirochetes

• chemotherapeutics: beta-lactam antibiotics: penicillins
• cell wall synthesis inhibitors

• penicillinase-resistant type: for staphylococcal infections (i.e. acute endocarditits and osteomyelitis), skin and soft tissue infections
• bacteria resistant to these are termed MRSA

• chemotherapeutics: beta-lactam antibiotics: penicillins
• cell wall synthesis inhibitors

• Extended-spectrum type:
• Aminopenicillins are used on streptococci and some enterococci; Amoxicillin largely used for RTI's (OM, sinusitis, bronchitis, community pneumonia).
• Antipseudomonal types (piperacillin...) are for a range of gram + and -
• All are becoming increasing combined with beta-lactase inhibitors (clavulanate, sulbactam).

• chemotherapeutics: beta-lactam antibiotics: cephalosporins
• cell wall synthesis inhibitors

• 1st Generation:
• cephalexin: skin/soft-tissue infections from gram + cocci
• cefazolin: for more serious infections, used as a surgical prophylactic for staph and gram - bacilli

• chemotherapeutics: beta-lactam antibiotics: cephalosporins
• cell wall synthesis inhibitors

• 2nd Generation:
• has the same action against gram + but increased activity against gram -

• chemotherapeutics: beta-lactam antibiotics: cephalosporins
• cell wall synthesis inhibitors

• 3rd generation:
• effective against a wider range of gram - bacilli
• Cefepime is aka a 4th generation as it is used against those that are resistant to other cephalosporins

• chemotherapeutics: beta-lactam antibiotics: Monobactam
• cell wall synthesis inhibitors

useful for infections caused by multi drug resistant strains

• chemotherapeutics: beta-lactam antibiotics: Carbapenems
• cell wall synthesis inhibitors

• penicillin-like, broad spectrum
• also good for multi drug resistant bacteria

chemotherapeutics: cell wall synthesis inhibitor

used to treat MRSA infections. Also good for C.diff,

• chemotherapeutics: inhibit protein synthesis
• Aminoglycosides

used with gram - or mycobacterial infections

• chemotherapeutics: inhibit protein synthesis
• Tetracyclines

• used on mycoplasma pneumonia
• can act bacteriocidal or bacteriostatic

chemotherapeutics: inhibit protein synthesis

used on MRSA and penicillin-resistant streptococci

• chemotherapeutics: inhibit protein synthesis
• Macrolide and Ketolide antibiotics

used on URTI's and pneumonia (community)

• chemotherapeutics: inhibit nucleic acid formation
• Fluoroquinolones

• respiratory infections (bronchitis, pneumonia, sinusitis, etc)
• urinary and gastro infections (cipro and levo)

• chemotherapeutics: inhibit nucleic acid formation
• Sulfonamides: antifolates (inhibit folic acid formation)

used on UTI's, burn/skin infections (silver sulfadiazine)

• chemotherapeutics: inhibit nucleic acid formation
• combined trimethoprim-sulfamethoxazole (TMP-SMX)

• trimethoprim can be used alone on prostatitis and vaginitis but is mainly combined with a sulfa drug to make it bacteriocidal and more potent
• used on UTI's and protatic infections, some resp infections (pneumocystitis carinii in AIDS)

• Anti-TB agents: 1st line drugs
• use in combinations: orders depend on degree on infection and +/- resistance to rifampin/isoniazid

• Anti-TB agents: 1st line drugs
• manufactured combinations

• Rifamate (Isoniazid + Rifampin)
• Rifater (Isoniazid + Rifampin + Pyrizinamide)

Anti-TB agents: 2nd line drugs

used in combinations in cases of resistant strains (or on pt's who are immunocompromized, i.e. Rifabutin)

• Anticoagulant (antithrombotic)
• Prevents venous thrombi formation; acts like Vit.K
• effects take days to develope

• Anticoagulant (antithrombotic)
• prevents venous thrombi formation; potentiates endogenous anticoagulant activity
• fast-acting

• Low molecular weight heparins
• anticoagulant (antithrombotic)
• prevent venous thrombi formation

longer duration of action than heparin

• Antiplatlet (antithrombotic), Non-Opiod Analgesic, anti-pyretic and anti-inflammatory
• A nonselective Cyclooxygenase inhibitor

use: pain, fever, inflammation, prophylaxis of MI, stroke and other thromboemolotic disorders.

• Antiplatlet (antithrombotic)
• used in conguntion with other anticoagulants
• keeps cAMP elevated, blocking platelet function

• Thrombolytic (antithrombotic)
• convert plasminogen to plasmin which digests fibrin and other coagulation factors

• use: acute MI
• streptokinase: emboli and DVT's

• anti-heparin agent
• binds with heparin so it can't bind the AT-III protein anymore.
• on its own, it can have anti-coagulant effects due to it's anti-platlet activity.

• Pulmonary vasodilator
• mimics prostaglandin, PGI2 or prostacyclin
• Autocoid

• selective dilation of pulmonary vessels used for PPHN or pulmonary HTN from high PVR
• also reduces platlet aggregation
• continuous infusion- life long therapy

• pulmonary vasodilator
• Type 5 PDI

• selective dilation of pulmonary vessels used for PPHN or pulmonary HTN from high PVR
• oral, IV or inhalational

pulmonary vasodilator

• selective dilation of pulmonary vessels used for PPHN or pulmonary HTN from high PVR
• *used for acute pulmonary HTN, refractory hypoxemia or post cardiac transplant

Crystalloid volume expanders

• use: hypotension due to plasma or blood loss
• preferred for fluid replacement

Colloid volume expanders

• use: hypotension due to plasma or blood loss
• preferred if there is extensive 3rd spacing fluid loss; have high oncotic pressures

blood products used as volume expanders

use: hypotension due to plasma or blood loss

Sedatives/Anxiolytics: Benzodiazepines (BZ)

• increase GABA at BZ receptora
• use: anxiety, EtOH withdrawal, muscle relaxant, anti-convulsive, amnesia and sleep

*Midazolam is used for conscious sedation (anethesia) and insomnia- preferred over barbiturates

• sedative/anxiolytic
• short-acting alpha-2 agonist

use: sedation of intubated patients. Provides "co-operative" sedation= no delirium and doesn't affect respiratory centers.

a benzodiazepine (BZ) antagonist

competetive antagonist, reverses BZ effects or OD

Hypnotics: Barbiturates

• Powerful (rarley used still)
• use: IV anesthesia, anti-convulsive, insomnia. Have anti-analgesic/hyperanalgesic effects and cause Resp depression

hypnotic

used for pediatric patients as it doesn't cause hyperanalgesia or paradoxical excitement

sedative-hypnotics

use: insomnia

IV anesthetic-hypnotic

• used in the OR and ICU for hypnotic properties. IV induction or pre-anesthetic sedation
• rapid emergence, less hangover effects

IV anesthetic-hypnotic

use: IV anesthetic for conscious sedation or RSI. for sedation/hypnotic effects without analgesia

IV anesthetic-hypnotic

• use: IV anesthetic, produces "dissociative anesthesia." Analgesia, reduced sensory perception, immobility and amnesia
• useful in children

hypnotic: phenothiazine

use: insomnia (esp in ICU with psychosis), anxiolytic, anagesic, neuralgia

Opioid anagesic

use: moderate to severe acute or chronic pain. nebulized morphine used to treat dyspnea in end-stage diseases.

opiods cause respiratory depression

opioid anagesic

• use: pain relief and cough supression.
• 10x stronger than morphine; rapid onset and faster duration of action with less hypnotic effects

opioid analgesic

use: cough supressant, mild-moderate pain (combined with other anagesics)

opioid anagesic

• use: second line agent for moderate to severe pain relief
• 1/10 the potency of morphine

opioid analgesic

use: maintenance of narcotic addicts during heroine or morphine withdrawal

opioid analgesic

• use: induction and maintenance of general anesthesia
• same effects as morphine but shorter duration and more potent. No adverse CNS effects

opioid analgesic

• use: adjuct to anesthsia or as an anesthetic. Useful in cardiac surgery due to its lack of cardiac effects
• 10x more potent than fentanyl

opioid analgesic

• use: anagesia and anethesia
• 3-5 min duration, decreases ICP, CMRO2 without touching CPP

Opioid antagonist (competetive)

causes immediate reversal of OD symptoms

Non-opioid analgesics: NSAIDS

• inhibit cyclooxygenase pathway (non-selective COX inhibitors)
• Asprin also has anti-inflammatory, anti-pyretic and anti-platelet properties
• Indocid is used to help close a PDA in neonates

Non-opioid analgesic: Para-aminophenol derrivatve

use: mild-moderate pain, anti-pyretic, works better on the CNS than the PNS

local anesthetics

• cocaine has good topical effects and its own vasoconstrictor
• lidocaine is a prototype: can be admin parenterally, orally and topically