20 19 Pharmacist's "Pharmacy Professional Knowledge I" high-frequency test center summarized the types of antibiotics.
(1) β -lactams: Penicillins and cephalosporins contain β -lactam rings in their molecular structures. Great progress has been made in recent years, such as thioenzyme, monolactone, β -lactonase inhibitor, methoxypenicillin and so on.
(2) Aminoglycosides: including streptomycin, gentamicin, kanamycin, tobramycin, amikacin, neomycin, ribomycin, micronomicin, astemycin, etc.
(3) Amide alcohols: including chloramphenicol, thiamphenicol, etc.
(4) Macrolides: erythromycin, leucomycin, odorless erythromycin, acetylspiramycin, midecamycin, josamycin and azithromycin are commonly used in clinic.
(5) Polypeptide antibiotics: vancomycin, norvancomycin and teicoplanin, the latter is superior to the former two in antibacterial activity, pharmacokinetics and safety.
(6) Other antibiotics acting on G- bacteria, such as polymyxin, fosfomycin, cyclosporine, cyclosporine, rifampicin, etc.
(7) Other antibiotics acting on G+ bacteria, such as lincomycin, clindamycin and bacitracin.
(8) Antifungal antibiotics: It can be divided into echinocandins, polyenes, pyrimidines, ergosterol antifungal drugs acting on fungal cell membranes, allylamines and azoospermia.
(9) Antitumor antibiotics: such as mitomycin, actinomycin D, bleomycin, adriamycin, etc.
Anti-tuberculosis bacteria: rifampicin, isoniazid, pyrazinamide, etc.
(1 1) cyclosporine and other immunosuppressive antibiotics.
Tetracyclines: including tetracycline, oxytetracycline, chlortetracycline and doxycycline.
20 19 professional knowledge of licensed pharmacists I classification of antipsychotic drugs in high-frequency test sites
According to the chemical structure, antipsychotic drugs can be divided into five categories:
1. phenothiazines-taking chlorpromazine hydrochloride as an example
Phenothiazides are an important class of antipsychotics. The basic structure of phenothiazine in its mother ring is a tricyclic compound connected by two benzene rings 1 main ring containing sulfur and nitrogen atoms. The three rings are not in the same plane, and the two benzene rings are folded into a plane bending angle α along the N-S axis (page 35). According to the different side chain groups, it can be divided into dimethylamine, piperazine and piperidine.
X-ray diffraction structure determination of chlorpromazine and dopamine shows that their conformations can partially overlap. In the conformation of chlorpromazine, the side chain tends to the direction of chlorine substituted benzene ring (see page 37, Figure 2- 15). The chlorine atom at the 2 nd position of chlorpromazine benzene ring causes molecular asymmetry, and the side chain inclines to the benzene ring side with chlorine atom, which is an important structural feature of this kind of drug molecules' antipsychotic effect. Without chlorine atoms, there is no antipsychotic effect. Chlorpromazine is a strong antipsychotic, but it has great toxic and side effects. In order to find new drugs with little toxic side effects and good curative effect, a lot of research work has been done on the structure-activity relationship of chlorpromazine, and its transformation law is as follows:
① The substitution of chlorine atom in position 2 is essential to the activity, and it is also effective to substitute with other electron-withdrawing groups. The stronger the electron-withdrawing effect of substituents, the stronger the activity, such as the substitution activity of trifluoromethyl is enhanced by 3-5 times. Substitution with weak electron-withdrawing groups will reduce activity and side effects, such as acetyl substitution.
② The sulfur atom at position 5 can be replaced by methylene, ethylene and ethylene, and it still has antipsychotic activity.
③ The nitrogen atom at the position of10 can be replaced by methylene, and still maintain its efficacy.
④ The side chain at 10 position can be replaced. For example, piperazine is used instead of dimethylamino to form a new type, and the activity is enhanced due to the improvement of oil-water distribution coefficient. For example, the antipsychotic effect of perphenazine is 6- 10 times that of chlorpromazine.
2. Thiophenes —— Take Chlorthiazide in Chlorthiazide as an example.
Its structure contains thioxanthene mother ring and alkaline side chain, which belongs to thiaanthracene antipsychotic drugs. It is another kind of antipsychotic drugs found in the structural transformation of phenothiazine, which replaces the nitrogen atom of phenothiazine ring with carbon atom and is connected with side chain through double bond. There are double bonds in the molecular structure of chlorprothixene, and the antipsychotic effect of cis-isomer and trans-isomer is 8 times that of trans-isomer, which may be due to the fact that cis-isomer can partially overlap dopamine molecules.
3. Butyl benzene-haloperidol
The chemical structure of this product is different from phenothiazine, but its pharmacological action and clinical use are similar. In order to overcome the shortcomings of this product and find drugs with good effect and low toxicity, a lot of structure-activity relationship studies have been carried out on these drugs, as shown in figure 2-2 1, and the structure has been reformed mainly around alkalinity, and the obtained drugs are shown in Mark 2- 15.
4. benzodiazepines
5. Other categories-Sulpiride
It is a benzamide antipsychotic found in the structural transformation of procainamide. This product selectively antagonizes D2, D3 and D4 receptors, and has antipsychotic and antiemetic effects. Compared with typical antipsychotic drugs, it has no sedative effect, no extrapyramidal reaction and few side effects.
Pharmacological effects of clozapine
Clozapine belongs to benzodiazepine antipsychotics. Clozapine has almost no extrapyramidal reaction. It mainly blocks dopamine receptors in limbic system, but has little effect on dopamine receptors in striatum.
Clozapine not only has a strong antipsychotic effect, but also has sedative, anticholinergic, adrenergic and antihistamine effects, which has a good effect on controlling acute symptoms such as agitation, hallucinations and delusions of psychosis, and also has a definite effect on patients with chronic withdrawal and passivity.
Licensed Pharmacist 20 19 Pharmaceutical Professional Knowledge-Classification of Three Tablets in High Frequency Test Center
1. Buccal tablets: refer to tablets that slowly dissolve in the mouth and produce local or systemic effects. The drugs in buccal tablets should be soluble, and mainly play the role of local anti-inflammation, sterilization, convergence, analgesia or local anesthesia.
2, sublingual buccal tablets: placed under the tongue can be quickly dissolved, the drug is absorbed by the sublingual mucosa, play a systemic role. Drugs and excipients in sublingual buccal tablets should be soluble and suitable for emergency treatment. It does not pass through the gastrointestinal tract and has no first-pass effect.
3. Oral patch: a tablet that is stuck in the oral cavity, absorbed by the mucosa, and acts locally or systemically.
4. Chewable tablets: tablets that are swallowed after chewing. Mannitol, sorbitol and sucrose should be selected as fillers and binders.
5. Soluble tablets: refers to uncoated tablets or film-coated tablets, which can be dissolved in water before use. Soluble tablets should be soluble in water, and the solution can be slightly milky white. Can be used for oral administration, external use, gargling, etc.
6. Effervescent tablets: tablets containing sodium bicarbonate and organic acids, which generate gas when meeting water and are effervescent. Organic acids include citric acid, tartaric acid and fumaric acid.
7. Vaginal tablets and vaginal effervescent tablets: tablets for vagina. Drugs that are not suitable for local stimulation. 8. Enteric-coated tablets: tablets coated with enteric materials.
Chemical properties of tetracycline drugs
Tetracycline antibiotics are a kind of broad-spectrum antibiotics and semi-synthetic antibiotics produced by actinomycetes, which have the basic skeleton of phenanthrene.
Tetracycline antibiotics are relatively stable at the initial stage, but will change color in the sun. It is not stable enough under acid and alkali conditions and is easy to hydrolyze. Tetracyclines mainly have the following chemical characteristics:
1. Unstable under acidic conditions: the hydrogen on C-6 hydroxyl group and C-5α is just in trans configuration, which is easy to eliminate the reaction and generate inactive orange dehydration.
Under the condition of pH 2-6, the dimethylamino group at C-4 position is easy to undergo reversible isomerization. Because of the hydrogen bond between C-5 hydroxyl group and C-4 dimethylamino group, the 4-position epimerization of oxytetracycline is more difficult than tetracycline. However, due to the steric repulsion of C-7 chlorine atom, the 4-position isomerization of chlortetracycline is more likely to occur than tetracycline.
2. Instability under alkaline conditions: isomers of lactone structure are generated under alkaline conditions.
3. Reaction with metal ions: It can form insoluble chelates with various metal ions under near-neutral conditions. This not only brings inconvenience to the clinical use of preparing suitable solution, but also interferes with the blood drug concentration during oral administration. Tetracycline can combine with calcium ions to form a complex. In vivo, the complex is yellow and deposited on bones and teeth. After children take it, teeth will turn yellow, and pregnant women may have tooth discoloration and bone growth inhibition after taking it. Therefore, children and pregnant women should use it with caution or disable it.
The Importance of 20 19 Pharmaceutical Formulation in the Pharmacy Professional Knowledge-High Frequency Examination Center of Licensed Pharmacists
(1) Different dosage forms change the action properties of drugs: Most drugs do not change their action properties after changing their dosage forms, but some drugs can change their action properties. For example, the oral dosage form of magnesium sulfate is used as a laxative, but intravenous drip of 5% injection can inhibit the central nervous system of the brain and has sedative and spasmolytic effects.
(2) Different dosage forms change the action speed of drugs, such as injection and inhalation aerosol. , quick effect, often used in first aid; Pills, sustained and controlled release preparations, implants, etc. Has slow action and belongs to a long-acting preparation.
(3) The toxic and side effects of different dosage forms: aminophylline has a good effect on asthma, but it has the toxic and side effects of accelerating the heartbeat. If made into suppository, this toxic side effect can be eliminated; The sustained and controlled release preparation created by Medical Education Network can keep the blood drug concentration stable and avoid the peak-valley phenomenon of blood drug concentration, thus reducing the toxic and side effects of drugs.
(4) Some dosage forms can produce targeted effects: intravenous injections with granular structure, such as liposomes, microspheres, microcapsules, etc. , enters the blood circulation system and is swallowed by macrophages in the reticuloendothelial system, so that drugs are concentrated in organs such as liver and spleen, and play a passive targeting role in liver and spleen.
(5) Some dosage forms affect the curative effect: Different preparation processes of solid dosage forms, such as tablets, granules, pills, etc., will have a significant impact on the curative effect, especially when the crystal form and particle size of the drug change, it will directly affect the drug release, thus affecting the therapeutic effect of the drug.
20 19 Pharmacist's "Pharmacy Professional Knowledge I" High Frequency Test Site 5 Aerosol Propellants and Additives
1.
Propellants can be generally divided into four categories: chlorofluoroalkanes, hydrofluoroalkanes, hydrocarbons and compressed gases. Propellant is the power to eject drugs, and sometimes it acts as a solvent for drugs. Propellants are mostly liquefied gas, whose boiling point is lower than room temperature under normal pressure. Therefore, it needs to be packed in pressure-resistant containers and controlled by valve system.
(1) hydrofluoroalkane: It is the most promising substitute for chlorofluoroalkane at present, including HFA- 134a (tetrafluoroethane) and HFA-227 (heptafluoropropane).
(2) Hydrocarbons: The main varieties are propane, n-butane and isobutane. Although this kind of propellant is stable, non-toxic, low density and low boiling point, it is flammable and explosive, which is not suitable for single application and is often mixed with chlorofluoroalkane propellant.
(3) Compressed gas: mainly carbon dioxide, nitrogen and nitric oxide. If this kind of non-liquefied compressed gas is filled at room temperature, the pressure will easily drop rapidly and the lasting injection effect will not be achieved.
2. cosolvent
3. Wetting agent
Quality requirements of implants
(1) Accessories used for implants must be biocompatible, and biodegradable materials such as silicone rubber can be used. The former should take out the materials after the scheduled time.
(2) The release rate of implants should be determined.
(3) Implant should be packaged in single dose, and the packaging container should be sterilized.
(4) The implant should be sealed and stored away from light.